(Hetero)Aryloxyaminopropanols with N-Phenylpiperazine Structural Fragment - Review of Cardiovascular Activity.
Abstract Aryloxyphenylpiperazinylpropanols are a group of compounds exhibiting a wide range of biological activities, affecting the central nervous system and many cardiovascular mechanisms among them. As cardiovascular agents, aryloxyphenylpiperazinylpropanols work as antihypertensives, antiarrhythmics, cardiotonics or antiaggregants. The mechanism of action is almost always an α1-adrenolytic or combined α1- and β-adrenolytic effect, but sometimes may be other mechanisms (e.g., Ca2+ antagonism or phosphodiesterase inhibition) can positively participate. In some cases, compounds with a small modif...
Source: Mini Reviews in Medicinal Chemistry - June 24, 2020 Category: Chemistry Authors: Marvanova P, Padrtova T, Mokry P Tags: Mini Rev Med Chem Source Type: research

Endophytic Fungi In The Fight Against Neglected Tropical Diseases.
Abstract Neglected tropical diseases are a serious global public health problem and they are one of the main causes of mortality and morbidity, especially in underdeveloped countries. These diseases have several implications for health and they are considered a priority in global eradication programs for disease control. The aim of this mini-review is to report recent studies on the fight against neglected diseases, namely dengue fever, chikungunya, zika, malaria protozoa, Chagas disease, leishmaniasis, schistosomiasis helminths, filariasis, and tuberculosis bacteria using extracts and isolated substances of endop...
Source: Mini Reviews in Medicinal Chemistry - June 24, 2020 Category: Chemistry Authors: Costa MBS, de Oliveira CM Tags: Mini Rev Med Chem Source Type: research

mTORC and PKC ε in Regulation of Alcohol Use Disorder.
mTORC and PKCε in Regulation of Alcohol Use Disorder. Mini Rev Med Chem. 2020 Jun 24;: Authors: Hanim A, Mohamed IN, Mohamed RMP, Das S, Nor NSM, Harun RA, Kumar J Abstract Alcohol use disorder (AUD) is characterized by compulsive binge alcohol intake, leading to various health and social harms. Protein Kinase C epsilon (PKCε), a specific family of PKC isoenzyme, regulates binge alcohol intake and potentiates alcohol-related cues. Alcohol via upstream kinases like mammalian target to rapamycin complex 1 (mTORC1) or 2 (mTORC2), may affect the activities of PKCε or vice versa in ...
Source: Mini Reviews in Medicinal Chemistry - June 24, 2020 Category: Chemistry Authors: Hanim A, Mohamed IN, Mohamed RMP, Das S, Nor NSM, Harun RA, Kumar J Tags: Mini Rev Med Chem Source Type: research

Association of micro RNA and Post-Operative Cognitive Dysfunction: A Review.
Abstract Postoperative Cognitive Dysfunction (POCD) refers to the condition of neurocognitive decline following a surgery in a cognitive and sensory manner. There are several risk factors, which may be life-threatening for this condition. Neuropsychological assessment of this condition is very important. In the present review, we discuss the association of apolipoprotein epsilon 4 (APOE ε4) and few miRNAs with POCD, and highlight the clinical importance for prognosis, diagnosis and treatment of POCD. Microarray is a genome analysis that can be used to determine DNA abnormalities. This current technique is ...
Source: Mini Reviews in Medicinal Chemistry - June 21, 2020 Category: Chemistry Authors: Yazit NAA, Juliana N, Das S, Teng NIMF, Effendy N, Azmani S, Kadiman S Tags: Mini Rev Med Chem Source Type: research

Effective Pharmacophore for CDC25 Phosphatases Enzyme Inhibitors: Newly Synthesized Bromothiazolopyrimidine Derivatives.
CONCLUSION: The novel bromothiazolopyrimidine derivatives showed promising in vitro anticancer activities against colon cancer HCT116 and lung cancer A549 cell lines comparable to the anticancer drug doxorubicin. PMID: 32560601 [PubMed - as supplied by publisher] (Source: Mini Reviews in Medicinal Chemistry)
Source: Mini Reviews in Medicinal Chemistry - June 19, 2020 Category: Chemistry Authors: El-Shahat M, Salama MAM, El-Farargy AF, Ali MM, Ahmed DM Tags: Mini Rev Med Chem Source Type: research

Monocyclic β-Lactam: A Review on Synthesis and Potential Biological Activities of a Multitarget Core.
Monocyclic β-Lactam: A Review on Synthesis and Potential Biological Activities of a Multitarget Core. Mini Rev Med Chem. 2020 Jun 19;: Authors: Leite THO, Saraiva MF, Pinheiro AC, de Souza MVN Abstract A monocyclic ring in their structure characterizes monobactams, a subclass of β-lactam antibiotics. Many of these compounds have a bactericidal mechanism of action and acts as penicillin and cephalosporins, interfering with bacterial cell wall biosynthesis. The synthesis of novel β-lactams is an emerging area of organic synthesis research due to the problem of increasing bacterial resista...
Source: Mini Reviews in Medicinal Chemistry - June 19, 2020 Category: Chemistry Authors: Leite THO, Saraiva MF, Pinheiro AC, de Souza MVN Tags: Mini Rev Med Chem Source Type: research

The Advances on the protective effects of ginsenosides on myocardial ischemia and ischemia-reperfusion injury.
Abstract Ginseng is a traditional medicine with a complex chemical composition, wide bioactivity and unique pharmacological action. Many studies have confirmed that ginsenosides are the active ingredients of ginseng, and ginsenosides have always been the focus of different researchers. With the development of modern separation and analysis technology, more than 150 kinds of ginsenosides have been isolated. The ginsenosides Rb1, Rb2, Rc, Rg1 and Re account for more than 80% of total ginsenosides, and other saponins, such as Rd, Rg3 and Rh2, which are minor constituents, account for only a small portion of the total...
Source: Mini Reviews in Medicinal Chemistry - June 19, 2020 Category: Chemistry Authors: Wang J, Wang H, Mou X, Luan M, Zhang X, He X, Zhao F, Meng Q Tags: Mini Rev Med Chem Source Type: research

Structure-activity Relationships of Natural and Synthetic Indole-derived Scaffolds as α-Glucosidase Inhibitors: A Mini-review.
Structure-activity Relationships of Natural and Synthetic Indole-derived Scaffolds as α-Glucosidase Inhibitors: A Mini-review. Mini Rev Med Chem. 2020 Jun 19;: Authors: Wang J, Lu S, Sheng R, Fan J, Wu W, Guo R Abstract α-Glucosidase plays an important role in carbohydrate metabolism and is an attractive drug target for the treatment of diabetes, obesity and other related complications. Currently, acarbose, miglitol and voglibose have been approved by FDA as treatment of diabetes by oral α-glucosidase inhibitors. With the development of anti-diabetic drugs, the emergence of novel dru...
Source: Mini Reviews in Medicinal Chemistry - June 19, 2020 Category: Chemistry Authors: Wang J, Lu S, Sheng R, Fan J, Wu W, Guo R Tags: Mini Rev Med Chem Source Type: research

Triterpenoid and saponin rich Phytolacca dodecandra L'Herit(Endod): A review on its phytochemistry and pharmacological properties.
Abstract Phytolacca dodecandra L'Herit (Endod) is the most extensively studied plant among 35 known species in the genus Phytolacca (Family: Phytolaccaceae). The plant has been used as a viable treatment for various ailments, such as malaria, rabies, ascariasis, and skin disorders, in many parts of Africa. In Ethiopia, the dried and powdered Endod berries have been used for a long period of time as a detergent to clean clothes. Since the discovery of the molluscicidal activities of its berries more than five decades ago, P. dodecandra has been a research focus worldwide and several phytochemicals mainly of triterp...
Source: Mini Reviews in Medicinal Chemistry - June 17, 2020 Category: Chemistry Authors: Desta KT, El-Aty AMA Tags: Mini Rev Med Chem Source Type: research

Synthesis, Characterization, Anti-proliferative Evaluation, and DNA Flow Cytometry Analysis of Some 2-Thiohydantoin derivatives.
CONCLUSION: Insertion of pyrazole, oxadiazole and, quinazoline moieties with 2-thiohydantoin moiety led to the enhancement of its anti-proliferative activity. Hence they can be used as anticancer agents. PMID: 32525773 [PubMed - as supplied by publisher] (Source: Mini Reviews in Medicinal Chemistry)
Source: Mini Reviews in Medicinal Chemistry - June 10, 2020 Category: Chemistry Authors: Elhady HA, Al-Shareef HF Tags: Mini Rev Med Chem Source Type: research

Ultrasmall Europium, Gadolinium, and Dysprosium Oxide Nanoparticles: Polyol Synthesis, Properties, and Biomedical Imaging Applications.
CONCLUSION: Unmixed, mixed, or doped ultrasmall Ln2O3 NPs with different Ln are extremely useful for in vivo imaging applications in MRI, CT, FI, MRI-CT, MRI-FI, CT-FI, and MRI-CT-FI. PMID: 32496986 [PubMed - as supplied by publisher] (Source: Mini Reviews in Medicinal Chemistry)
Source: Mini Reviews in Medicinal Chemistry - June 4, 2020 Category: Chemistry Authors: Yue H, Park JY, Chang Y, Lee GH Tags: Mini Rev Med Chem Source Type: research

Performance evaluation of docking programs- Glide, GOLD, AutoDock & SurflexDock, using free energy perturbation reference data: A case study of fructose-1, 6-bisphosphatase-AMP analogs.
Performance evaluation of docking programs- Glide, GOLD, AutoDock & SurflexDock, using free energy perturbation reference data: A case study of fructose-1, 6-bisphosphatase-AMP analogs. Mini Rev Med Chem. 2020 May 26;: Authors: Reddy KK, Rathore RS, Srujana P, Burri RR, Reddy CR, Sumakanth M, Reddanna P, Reddy MR Abstract The accurate ranking of analogs of lead molecules with respect to their estimated binding free energies to drug targets remains highly challenging in molecular docking due to small relative differences in their free energy values. Free energy perturbation (FEP) method, which prov...
Source: Mini Reviews in Medicinal Chemistry - May 26, 2020 Category: Chemistry Authors: Reddy KK, Rathore RS, Srujana P, Burri RR, Reddy CR, Sumakanth M, Reddanna P, Reddy MR Tags: Mini Rev Med Chem Source Type: research

Discovering the Potentials of Medicinal Mushrooms in Combating Depression - A Review.
Abstract Depression is the most common form of mental illness and the major cause of disability worldwide. Symptoms of depression including feelings of intense sadness and hopelessness may occur after a specific event or in response to a gradual decline in health and functional status, often associated with ageing. Current therapies for treating these symptoms include antidepressant drugs, counseling and behavioral therapy. However, antidepressant drugs are associated with mild to severe adverse effects, which has prompted the need for better treatment options. Medicinal mushrooms are valuable sources of food and ...
Source: Mini Reviews in Medicinal Chemistry - May 26, 2020 Category: Chemistry Authors: Lew SY, Teoh SL, Lim SH, Lim LW, Wong KH Tags: Mini Rev Med Chem Source Type: research

Current Progress in Biomedical Applications of Chitosan-Carbon Nanotube Nanocomposites: A Review.
Abstract The currently observed development of medical science results from the constant search for innovative solutions to improve the health and quality of life of patients. Particular attention is focused on the design of a new generation of materials with a high degree of biocompatibility and tolerance towards the immune system. In addition, apart from biotolerance, it is important to ensure appropriate mechanical and technological properties of materials intended for intrabody application. Knowledge of the above parameters becomes the basis for considerations related to the possibilities of choosing the appro...
Source: Mini Reviews in Medicinal Chemistry - May 13, 2020 Category: Chemistry Authors: Pieklarz K, Modrzejewska Z Tags: Mini Rev Med Chem Source Type: research

New strategies for safe cancer therapy using electrospun nanofibers: A short review.
Abstract Electrospun nanofibers regarding to their special features including high drug loading capacity, high surface to volume area, flexibility and ease of production and operation are of great interest for being used in tissue engineering and drug delivery approaches. In this context several studies have been done for production of biodegradable and biocompatible scaffolds containing different anticancer agents for fighting with solid tumors. Surprisingly these scaffolds are able to deliver different combinations of drugs and agents such as nanoparticles and release them in time dependent manner. Here in this ...
Source: Mini Reviews in Medicinal Chemistry - May 13, 2020 Category: Chemistry Authors: Doostmohammadi M, Forootanfar H, Ramakrishna S Tags: Mini Rev Med Chem Source Type: research

Irreversible kinase inhibitors targeting to cysteine residues and their applications in cancer therapy.
Abstract Protein kinases are the conserved enzymes that catalyze the phosphorilation process in cells and recognized as the targets for many diseases. FDA has approved many kinase inhibitors for the treatment of cancer and confirmed kinases as the relevant targets for drug discovery. Major approved drugs are ATP competitive reversible non-covalent inhibitors that achieve selectivity by recognition of specific binding pocket of the targeted kinases. In recent years scientists have paid more attention in the development of irreversible covalent kinase inhibitors to achieve better selectivity, less toxicity and side ...
Source: Mini Reviews in Medicinal Chemistry - May 13, 2020 Category: Chemistry Authors: Das D, Hong J Tags: Mini Rev Med Chem Source Type: research

A Systematic Review of Current Progresses in The Nucleic Acid-Based Therapies for Neurodegeneration with Implications for Alzheimer's disease.
CONCLUSION: With recent successes in the systemic delivery of nucleic acids via intravenous injection; it is worth investing in the production of new-generation medicines. There are still several challenges for NA-BTs including, their delivery to the effective modulators, mass production at low cost, sustaining efficacy and minimizing off-target effects. Regarding miRNA-based therapies, given the obvious involvement of miRNAs in numerous facets of brain disease, and the many sophisticated techniques for delivery to the brain, miRNA-based therapies will make new hope for the treatment of neurological diseases such as AD. ...
Source: Mini Reviews in Medicinal Chemistry - May 13, 2020 Category: Chemistry Authors: Ghaffari M, Sanadgol N, Abdollahi M Tags: Mini Rev Med Chem Source Type: research

Nano-strategies for Improving the Bioavailability of Inhaled Pharmaceutical Formulations.
Abstract Pulmonary pharmaceutical formulations are targeted for the treatment of respiratory diseases. However, their application is limited due to physiological characteristics of the lungs such as branching structure, mucociliary and macrophages, as well as certain properties of the drugs like particle size and solubility. Nano-formulations can ameliorate particle sizes and improve drug solubility to enhance bioavailability in the lungs. The nano-formulations for lungs reviewed in this article can be classified into nanocarriers, no-carrier-added nanosuspensions and polymer-drug conjugates. Compared with convent...
Source: Mini Reviews in Medicinal Chemistry - May 9, 2020 Category: Chemistry Authors: Xing Y, Lu P, Xue Z, Liang C, Zhang B, Kebebe D, Liu H, Liu Z Tags: Mini Rev Med Chem Source Type: research

Recent Developments of Target Based Coumarin Derivatives as Potential Anticancer Agents.
Abstract Cancer is the second life-threatening disease worldwide, and it results in around 9.6 million deaths globally in 2018. The multidrug-resistant cancers and non-selectivity create an urge for the development of novel anticancer drugs with diverse mechanism of action. Coumarin is one of the most widely used scaffolds for the development of highly effective anticancer agents. It has versatile anticancer profiles with diverse mechanisms to inhibit tumor progression. The facile synthetic strategies are also favoured for target based coumarin derivatives. Structural Activity Relationship (SAR) studies determine ...
Source: Mini Reviews in Medicinal Chemistry - May 9, 2020 Category: Chemistry Authors: Goud NS, Kumar P, Bharath RD Tags: Mini Rev Med Chem Source Type: research

Recent Advances in the Development of "Curcumin Inspired" Compounds as New Therapeutic Agents.
Recent Advances in the Development of "Curcumin Inspired" Compounds as New Therapeutic Agents. Mini Rev Med Chem. 2020 May 07;: Authors: Borosky GL, Laali KK Abstract Despite a huge body of research in the past two decades investigating the antioxidant, anti-inflammatory, antimicrobial, and anti-carcinogenic properties of curcumin (CUR), a CUR-based anti-tumor drug is yet to be developed. Lack of success in achieving this goal stems from CUR's unfavorable biophysicochemical features, particularly poor solubility, low bioavailability, and rapid metabolism, coupled to a complex biological prof...
Source: Mini Reviews in Medicinal Chemistry - May 7, 2020 Category: Chemistry Authors: Borosky GL, Laali KK Tags: Mini Rev Med Chem Source Type: research

Pharmacological and Therapeutic Aspects of Plants from the Genus Ferula: a Comprehensive Review.
Abstract Inspired by nature, humankind has been able to attain significant achievements in the drug and food industries. Particularly, medicinal plants are a rich source of medicinal, cosmetic, sanitary, and aromatic substances. Genus Ferula from Apiaceae family is a plant genus that possesses over 170 species, which have been carefully documented with regard to their medicinal properties. Ferula spp. affect many body organs, and their respective functions, in humans, such as the immune system, gastrointestinal tract, genitourinary, endocrine, respiratory, cardiovascular, nervous system, bone (skeleton), and teeth...
Source: Mini Reviews in Medicinal Chemistry - May 5, 2020 Category: Chemistry Authors: Sabzehzari M, Naghavi MR, Bozari M, Orafai H, Johnston TP, Sahebkar A Tags: Mini Rev Med Chem Source Type: research

Anticancer and Antimicrobial Activities of Naproxen and Naproxen Derivatives.
l;kgüzel ŞG Abstract This review explains the effects of naproxen and containing the naproxen moiety in important biological activities. Naproxen, 2-(6-methoxynaphthalen-2-yl)propionic acid, is one of the most utilized propionic acid derivatives to the cure of many injuries or pains. Naproxen is a non-steroidal anti-inflammatory drug (NSAID), which is generally using among the NSAIDs. Even though gastrointestinal side effects, naproxen has been safely used for many years because of the good cardiovascular sight. In last years, except for anti-inflammatory effects other pharmacological activities of naproxen,...
Source: Mini Reviews in Medicinal Chemistry - May 5, 2020 Category: Chemistry Authors: Han Mİ, Küçükgüzel ŞG Tags: Mini Rev Med Chem Source Type: research

Synthesis, Characterization, Antimicrobial and Anticancer Studies of Metal Complexes of 2-methoxy-4-((3-methylpyridin-2-ylimino)methyl)phenol.
Abstract Being derived from primary amine and aromatic aldehyde, Schiff base and their complexes have an imperative role in the improvement of inorganic chemistry which are broadly studied as coordination compounds and are gradually becoming more important in biochemical and analytical applications. They have also been used for antibacterial, antifungal, anticancer, antitubercular activities. Novel synthesised Schiff's base 2-methoxy-4-((3-methylpyridin-2-ylimino)methyl)phenol (SB) and its metal complexes (Zn[II], Cu[II], Co[II] and Ni[II]) were characterised by UV, IR and NMR spectroscopy. Formation of the Schiff...
Source: Mini Reviews in Medicinal Chemistry - May 5, 2020 Category: Chemistry Authors: Mishra A, Tahlan S, Ramasamy K, Lim SM, Shah SAA, Narasimhan B Tags: Mini Rev Med Chem Source Type: research

Andrographolide: Synthetic Methods and Biological Activities.
Abstract Andrographolide, a labdane diterpenoid, is extracted and isolated from the plants of Andrographis paniculata. Andrographolide and its derivatives exhibited a wide range of biological properties including anticancer activity, antibacterial activity, hepatoprotective activity, anti-inflammatory activity, antiviral activity, anti-malarial activity, antidiabetic activity, insecticidal activity, etc. As a continuation, this review aims at giving an overview on the update advances (from 2015 to 2018) of andrographolide and it derivatives in regard to bioactivities, mechanisms of action, structural modifications...
Source: Mini Reviews in Medicinal Chemistry - April 28, 2020 Category: Chemistry Authors: Hao M, Xu H Tags: Mini Rev Med Chem Source Type: research

Psoralen: A Biological Important Coumarin with Emerging Applications.
Abstract Coumarin has a place with a class of lactones which are fundamentally comprising of a benzene ring fused to αpyrone ring, known as benzopyrones. It likewise has a conjugated framework with electron rich and good charge-transport properties. It is delivered by plants to shield themselves from predation as a chemical response. Despite the fact that, coumarins have been utilized in different products like cosmetics, additives, perfumes, aroma enhancers in various tobaccos and some alcoholic drinks their most relevant role in natural products, organic and medicinal chemistry. Besides, as medicinal candi...
Source: Mini Reviews in Medicinal Chemistry - April 28, 2020 Category: Chemistry Authors: Thakur A, Sharma R, Jaswal VS, Nepovimova E, Chaudhary A, Kuca K Tags: Mini Rev Med Chem Source Type: research

p-Benzoquinone a privileged scaffold of pharmacological significance: A review.
Abstract Quinones are a huge class of compounds capable with affluent and captivating chemistry. p-Benzoquinone (pBNZ) or 1,4-Benzoquinone is a quinone compound which is the key structural motif of numerous biologically active molecules including synthetic and natural products that craft interest in its biological exploration to assess their prospective therapeutic implication. It acquires immense therapeutic potential with least side effects based on the different substitutions on this core molecule. This moiety has a marvelous capability to regulate a varied range of different cellular pathways that can be inves...
Source: Mini Reviews in Medicinal Chemistry - April 28, 2020 Category: Chemistry Authors: Silakari P, Chhikara P, Piplani P Tags: Mini Rev Med Chem Source Type: research

The Impact of Plant Bioactive Compounds on Aging and Fertility of Diverse Organisms: A Review.
Abstract It is expected that in 2050 there will be more than 20% of senior citizens aged over 60 years worldwide. Such alarming statistics require immediate attention to improve the health of the aging population. Since aging is closely related to the loss of antioxidant defense mechanism, this situation will eventually lead to numerous health problems, including fertility reduction. Furthermore, plant extracts were used in traditional medicine as potent antioxidant sources. Despite many experiments had reported the impact of various bioactive compounds on aging or fertility, there is lack of review papers which c...
Source: Mini Reviews in Medicinal Chemistry - April 28, 2020 Category: Chemistry Authors: Noordin MAM, Noor MM, Aizat WM Tags: Mini Rev Med Chem Source Type: research

Applications Quantitative Structure-Activity Relationships (QSAR) based Virtual Screening in drug design: A Review.
Abstract Today, the scientific community across the globe generates huge data; for example more than 74 million substances are registered in Chemical Abstract Services. Another estimate tells that there is about 1060 molecules classified as new drug like molecules. This huge space is now refereed as 'dark chemical space' or 'dark chemistry'. Today one can see a surge in the number live databases (protein, cell, tissues, structure, drugs etc.) and every day these are updated with new information. So, the synchronization of the three different sciences 'genomics', proteomics' and 'in-silico simulation' is essential ...
Source: Mini Reviews in Medicinal Chemistry - April 28, 2020 Category: Chemistry Authors: Achary PGR Tags: Mini Rev Med Chem Source Type: research

Tanshinones and their derivatives: heterocyclic ring-fused diterpene of biological interest.
ero I, Marrero JG Abstract The available scientific literature regarding tanshinones is very abundant, and after its review, it is noticeable that most of the articles focus on the properties of tanshinone I, cryptotanshinone, tanshinone IIA, sodium tanshinone IIA sulfonate and the dried root extract of Salvia miltiorrhiza (Tan-Shen). However, although these products have demonstrated important biological properties in both in vitro and in vivo models, their poor solubility and bioavailability have limited their clinical applications. For these reasons, many studies have focused on the search for new pharmaceutica...
Source: Mini Reviews in Medicinal Chemistry - April 28, 2020 Category: Chemistry Authors: Estolano-Cobián A, Alonso MM, Díaz-Rubio L, Ponce CN, Córdova-Guerrero I, Marrero JG Tags: Mini Rev Med Chem Source Type: research

Current Trends in Drug Delivery System of Curcumin and its Therapeutic Applications.
This article delivers a general idea of the current study piloted to overwhelm the complications with the bioavailability of curcumin which have exhibited an enhanced biological activity than curcumin. This article explains the latest and detailed study of curcumin and its conjugates, its phytochemistry, and biological perspectives and also proved curcumin as an efficient drug candidate for the treatment of numerous diseases. Recent advancements and futuristic viewpoints are also deliberated which shall help researchers and foster commercial translations of improved nano-sized curcumin combination for the treatment of vari...
Source: Mini Reviews in Medicinal Chemistry - April 28, 2020 Category: Chemistry Authors: Sethiya A, Agarwal DK, Agarwal S Tags: Mini Rev Med Chem Source Type: research

Traditional Uses, Therapeutic Effects and Recent Advances of Curcumin: A Mini-Review.
In conclusion, curcumin is widely used for myriad therapeutic purposes that trigger its significant value. This short review aims to highlight the known biological activities of curcumin and provide evidence for its antitumor effects. PMID: 32286941 [PubMed - as supplied by publisher] (Source: Mini Reviews in Medicinal Chemistry)
Source: Mini Reviews in Medicinal Chemistry - April 14, 2020 Category: Chemistry Authors: Slika L, Patra D Tags: Mini Rev Med Chem Source Type: research

Zinc Poisoning - Symptoms, Causes, Treatments.
Abstract Zinc poisoning has been reported from many parts of the world. It is one of the global health problems that affect many organs if consume or expose by inhalation of zinc vapors or zinccontaminated water and food. Long term exposure to zinc compounds from different sources such as; air, water, soil, and food lead to toxic effects on body systems especially digestive, respiratory, and nerve systems and also causes cancer. Zinc levels can be determined in blood, urine, hair and nails. Patients with zinc toxicity need chelating agents, other pharmacological treatment, protective lung ventilation, extracorpore...
Source: Mini Reviews in Medicinal Chemistry - April 14, 2020 Category: Chemistry Authors: Rahimzadeh MR, Rahimzadeh MR, Kazemi S, Moghadamnia AA Tags: Mini Rev Med Chem Source Type: research

Anti-DENV And Anti-Dengue Vector Activity of Some Heterocyclic Scaffolds.
Abstract Dengue is a major health threat related to arbovirus and is endemic in more than 100 countries with an annual estimated above 390 million incidences of infection all around the world. During the period 1996-2015, a considerable increase in number of dengue cases (more than 500%) was reported in India. Information about dengue disease burden, its prevalence, incidence and geographic distribution is critical in planning appropriate control measures against dengue fever. Till date, no specific treatment for dengue fever is available in any system of medicine which can be accepted globally. Therefore, safe, c...
Source: Mini Reviews in Medicinal Chemistry - April 14, 2020 Category: Chemistry Authors: Purohit D, Dhingra N, Dutt R, Kumar S Tags: Mini Rev Med Chem Source Type: research

Secretory Clusterin: A Promising Target for Chemoresistance of Hepatocellular Carcinoma.
Abstract Hepatocellular carcinoma (HCC) is a leading cause of cancer-related deaths worldwide. Chemoresistance remains the major factor for the limited efficacy of HCC treatment. Thus, exploring the mechanisms underlying drug resistance is of great importance. Secretory clusterin (sCLU), a stress-activated and ATP-independent molecular chaperone, is up-regulated in numerous tumors and correlated with malignant phenotypes. For HCC, the implication of sCLU was previously addressed in the tumor growth, metastasis, as well as the early diagnosis and poor prognosis. Notably, accumulating studies have emphasized its vit...
Source: Mini Reviews in Medicinal Chemistry - March 30, 2020 Category: Chemistry Authors: Zhang J, Wu M, Xu Y, Song Q, Zheng W Tags: Mini Rev Med Chem Source Type: research

Antiviral drug discovery and development for Mayaro Fever - What do we have so far?
Abstract Tropical infectious diseases cause millions of deaths every year in developing countries with about half of the world population living at risk. Mayaro virus (MAYV) is an emerging arbovirus that causes Mayaro fever, which is characterized by fever, headache, diarrhea, arthralgia and rash. These symptoms can be clinically indistinguishable from other arboviruses, such as Dengue, Zika and Chikungunya, which makes the diagnosis and treatment of the disease more difficult. Though, Mayaro virus is a potential candidate to cause large-scale epidemics on the scale of ZIKV and CHIKV. Despite this, there is no lic...
Source: Mini Reviews in Medicinal Chemistry - March 16, 2020 Category: Chemistry Authors: de Mello MV, Domingos TF, Ferreira D, Ribeiro M, Ribeiro T, Souza A, Rodrigues C Tags: Mini Rev Med Chem Source Type: research

An appraisal of current pharmacological perspectives of sesamol: A review.
CONCLUSION: In the present review, pharmacological effects of sesamol are summarized with the available mechanistic data. Several pharmacological effects of sesamol are reported namely, anti-oxidant, anti-cancer, neuroprotective, cardioprotective, anti-inflammatory, hypolipidemic, radioprotective, anti-aging, anti-ulcer, anti-dementia, anti-depressant, antiplatelet, anticonvulsant, anti-anxiolytic, wound healing, cosmetic (skin whitening), anti-microbial, Matrix metalloproteinase (MMPs) inhibition, hepatoprotective activity and other biological effects. Here we have summarized the proposed mechanism behind these pharmacolo...
Source: Mini Reviews in Medicinal Chemistry - March 13, 2020 Category: Chemistry Authors: Bosebabu B, Cheruku SP, Chamallamudi MR, Nampoothiri M, Shenoy RR, Nandakumar K, Parihar VK, Kumar N Tags: Mini Rev Med Chem Source Type: research

The role of the cannabinoid system in opioid analgesia and tolerance.
Abstract Opioid receptor agonist drugs, such as morphine, are very effective for treating chronic and severe pain; but, tolerance can develop with long-term use. Although there is a lot of information about the pathophysiological mechanisms of opioid tolerance, it is still not fully clarified. Suggested mechanisms for opioid tolerance include opioid receptor desensitisation, reduction of sensitivity G-proteins, activation of mitogen-activated protein kinase (MAPK), altered intracellular signaling pathway including nitric oxide, and activation of mammalian target of rapamycin (mTOR). One way to reduce opioid tolera...
Source: Mini Reviews in Medicinal Chemistry - March 13, 2020 Category: Chemistry Authors: Ozdemir E Tags: Mini Rev Med Chem Source Type: research

Inhibitor binding sites in the protein tyrosine phosphatase SHP-2.
Abstract Protein tyrosine phosphatase 2 (SHP-2) has long been proposed as a cancer drug target. Several small molecule compounds with different mechanisms of SHP-2 inhibition have been reported, but none are commercially available. Pool selectivity over protein tyrosine phosphatase 1 (SHP-1) and a lack of cellular activity have hindered the development of selective SHP-2 inhibitors. In this review, we describe the binding modes of existing inhibitors and SHP-2 binding sites, summarize the characteristics of the sites involved in selectivity, and identify the suitable groups for interaction with the binding sites. ...
Source: Mini Reviews in Medicinal Chemistry - March 3, 2020 Category: Chemistry Authors: Zhang H, Gao Z, Meng C, Li X, Shi D Tags: Mini Rev Med Chem Source Type: research

Single heterocyclic compounds as Monoamine Oxidase Inhibitors: From past to present.
Abstract Inhibitors of monoamine oxidase (MAO) have shown therapeutic values in a variety of neurodegenerative diseases such as depression, Parkinson's disease and Alzheimer's disease. Heterocyclic compounds exhibit a broad spectrum of biological activities and vital leading compounds for the development of chemical drugs. Herein, we focus on the synthesis and screening of novel single heterocyclic derivatives with MAO inhibitory activities during the past decade. This review covers recent pharmacological advancements of single heterocyclic moiety along with structure activity relationship so as to provide better ...
Source: Mini Reviews in Medicinal Chemistry - March 1, 2020 Category: Chemistry Authors: Wu SM, Qiu XY, Liu SJ, Sun J Tags: Mini Rev Med Chem Source Type: research

Review on Chemistry, Analysis, and pharmacology of teneligliptin: a novel DPP-4 inhibitor.
This article provides comprehensive and collective facts about teneligliptin. Teneligliptin is a dipeptide peptidase-4 (DPP-4) inhibitor belongs to the third generation, used in the management of type 2 diabetes. It inhibits human DPP-4 enzyme activity. This drug falls under class 3 as it interacts with the extensive sub-sites like S1, S2, and S2E. Teneligliptin and its metabolites mainly determined in human plasma matrix by hyphenated chromatographic methods. Theses developed methods could be foreseen for its clinical applications. Moreover, the stress degradation studies of teneligliptin under stress conditions along wit...
Source: Mini Reviews in Medicinal Chemistry - February 28, 2020 Category: Chemistry Authors: Sharma S, Sharma R, Hatware K, Patil K Tags: Mini Rev Med Chem Source Type: research

Botulinum toxin as biological warfare agent: poisoning, diagnosis and countermeasures.
Abstract Botulinum toxin is a neurotoxin produced by Clostridium botulinum and some other relative species. It causes lethal disease called botulism. It can enter body via infections by Clostridium (e.g. wound and children botulism) or by a direct contact with the toxin or eating a contaminated food (food-borne botulism). Botulinum toxin is also considered as a relevant biological warfare agent with expected high number of causalities when misused for bioterrorist or military purposes. The current paper surveys the actual knowledge about botulinum toxin pathogenesis, manifestation of poisoning, current trends in d...
Source: Mini Reviews in Medicinal Chemistry - February 27, 2020 Category: Chemistry Authors: Pohanka M Tags: Mini Rev Med Chem Source Type: research

Medicinal Potential of Heterocyclic Compounds from Diverse Natural Sources for the Management of Cancer.
Abstract Natural products form a significant portion of medicinal agents that are currently used for the management of cancer. All these natural products have unique structures along with diverse action mechanisms with the capacity to interact with different therapeutic targets of several complex disorders. Although the plants contribute as a major source of natural products with anti-cancer potential, the marine environment and microbes have also bestowed some substantial chemotherapeutic agents. Few examples of anti-cancer agents of natural origin include vincristine, vinblastine, paclitaxel, camptothecin and to...
Source: Mini Reviews in Medicinal Chemistry - February 11, 2020 Category: Chemistry Authors: Singh M, Sharma P, Singh PK, Singh TG, Saini B Tags: Mini Rev Med Chem Source Type: research

Anticancer agents based on vulnerable components in a signalling pathway.
Abstract Traditional cancer treatment includes surgery, chemotherapy, radiotherapy and immunotherapy that are beneficially clinically, but are associated with drawbacks such as drug resistance and side effects. In quest of better treatment many new molecular targets have been introduced in the last few decades. Finding new molecular mechanisms encourages researchers to discover new anticancer agents. Exploring the mechanism of action also facilitates both anticipation of potential resistance mechanisms and optimization of rational combination therapies. The write up describes the leading molecular mechanisms for c...
Source: Mini Reviews in Medicinal Chemistry - February 11, 2020 Category: Chemistry Authors: Vaidya A, Jain S, Sahu S, Jain PK, Pathak K, Pathak D, Kumar R, Jain SK Tags: Mini Rev Med Chem Source Type: research

Lignans from medicinal plants and their anticancer effect.
Abstract Since early times, various plants have been used as remedies for treating different kinds of diseases and lesions with satisfying results. The phenolic compounds are secondary metabolites from medicinal plants which include a wide category of compounds such as phenolic acids, flavonoids, tannins, stilbenes, curcuminoids, xanthones, coumarins, lignans, etc. Between these, lignans are considered important in cancer prevention and treatment, besides others beneficial health effects, e.g. antioxidant, anticarcinogenic, antimutagenic and anti-estrogenic effects. This review summarizes the most recent literatur...
Source: Mini Reviews in Medicinal Chemistry - February 11, 2020 Category: Chemistry Authors: Teodor ED, Moroeanu V, Radu GL Tags: Mini Rev Med Chem Source Type: research

The application of combination of Monte Carlo optimization method based QSAR modeling and molecular docking in drug design and development.
Abstract In recent years as one of the promising approaches in QSAR modeling Monte Carlo optimization approach as conformation independent method has emerged. Monte Carlo optimization has proven to be valuable tool in chemoinformatics and this review presents its application in drug discovery and design. In this review the basic principles and important features of these methods are discussed as well as the advantages of conformation independent optimal descriptors developed from molecular graph and Simplified Molecular Input Line Entry System (SMILES) notation compared to commonly used descriptors in QSAR modelin...
Source: Mini Reviews in Medicinal Chemistry - February 11, 2020 Category: Chemistry Authors: Zivkovic M, Zlatanovic M, Zlatanovic N, Golubović M, Veselinović AM Tags: Mini Rev Med Chem Source Type: research

Prospective application of aptamer-based assays and therapeutics in bloodstream infections.
Abstract Sepsis is still a severe health problem worldwide with high morbidity and mortality. Blood bacterial culture remains the gold standard for detection of pathogenic bacteria in bloodstream infections but time-consuming and both of the sophisticated equipment and well-trained personnel are required. Immunoassays and genetic diagnosis are expensive and limited to specificity and sensitivity. Aptamers are single-stranded deoxyribonucleic acid (ssDNA) and ribonucleic acid (RNA) oligonucleotide or peptide sequence generated in vitro based on binding affinity of aptamer-target by a process known as Systematic Evo...
Source: Mini Reviews in Medicinal Chemistry - February 11, 2020 Category: Chemistry Authors: Li W Tags: Mini Rev Med Chem Source Type: research

The QSAR Paradigm in Fragment-Based Drug Discovery: From the Virtual Generation of Target Inhibitors to Multi-Scale Modeling.
CONCLUSION: As huge amounts of data continue to accumulate in the domains of the chemical, biological and biomedical sciences, it has become clear that drug discovery must be viewed as a multi-scale optimization process. An ideal multi-scale approach should integrate diverse chemical and biological data and also serve as a knowledge generator, enabling the design of potentially optimal chemicals that may become therapeutic agents. PMID: 32013845 [PubMed - as supplied by publisher] (Source: Mini Reviews in Medicinal Chemistry)
Source: Mini Reviews in Medicinal Chemistry - February 4, 2020 Category: Chemistry Authors: Kleandrova VV, Speck-Planche A Tags: Mini Rev Med Chem Source Type: research

Medicinal Chemistry Meets Electrochemistry: Redox Potential in the Role of Endpoint or Molecular Descriptor in QSAR/QSPR.
e;k K Abstract Many biochemical reactions are based on redox reactions, therefore the redox potential of a chemical compound may be related to its therapeutic or physiological effects. Study of redox properties of com-pounds is a domain of electrochemistry. The subject of this review is the relationship between electro-chemistry and medicinal chemistry, with a focus on quantifying these relationships. A summary of the relevant achievements in the correlation between redox potential and structure, therapeutic activity, resp., is presented. The first part of the review examines the applicability of QSPR for predicti...
Source: Mini Reviews in Medicinal Chemistry - February 4, 2020 Category: Chemistry Authors: Nesměrák K Tags: Mini Rev Med Chem Source Type: research

Consensus analyses in molecular docking studies applied to medicinal chemistry.
Abstract The increasing number of computational studies in medicinal chemistry involving molecular docking has put the technique forward as promising in the design of Computer-Aided Drug Design. Considering the main method in the virtual screening based on the structure, consensus analysis of docking has been applied in several studies to overcome limitations of algorithms of different programs and mainly to increase the reliability of the results and reduce the number of false positives. However, some consensus scoring strategies are difficult to apply and in some cases are not reliable because of the small numbe...
Source: Mini Reviews in Medicinal Chemistry - February 4, 2020 Category: Chemistry Authors: Maia MDS, Soares Rodrigues GC, Silva Cavalcanti AB, Scotti L, Scotti MT Tags: Mini Rev Med Chem Source Type: research

Through Biological Control to Reduce the Disease Burden of Human Schistosomiasis in Asia.
Abstract Schistosomiasis is a chronic parasitic disease caused by a trematode blood fluke of the genus Schistosoma that belongs to the Schistosomatidae family. It is a neglected disease in different regions of Asia. In this review 218 articles (between 2000 and 2017) related to topic was collected from PubMed and Google scholar and reviewed. After thoroughly reading of collected articles due to not met topic requirement the 94 articles were excluded. Articles that have data associated with Asian regions are considered. In Asia, the disease is prevalent in China, Philippines, Indonesia, Yemen, Nepal and Laos etc. W...
Source: Mini Reviews in Medicinal Chemistry - February 3, 2020 Category: Chemistry Authors: Saleem S, Ahmed H, Siddiqui T, Kilinc SG, Khan A, Afzal MS, Simsek S Tags: Mini Rev Med Chem Source Type: research