Targeting Integrase enzyme: A Therapeutic Approach to combat HIV resistance.
Abstract Global HIV statistics by World Health Organization (WHO) for the year 2017 was estimated to be 36.9 (31.1-43.9) million. Antiviral drug resistance poses a serious threat to the public health and requires immediate action. Retroviral integrase (IN) a component enzyme in the retroviral pre-integration complex (PIC) enables a retrovirus to incorporate its genetic material into the host DNA. Development of resistance to the current integrases invites immediate attention of the drug discovery community for the development of new second-generation INtegrase Strand Transfer Inhibitors (INSTIs), the need of hour ...
Source: Mini Reviews in Medicinal Chemistry - October 15, 2019 Category: Chemistry Authors: Komal D, Joshi K, Sethi A, Soukya L, Alvala M Tags: Mini Rev Med Chem Source Type: research

Design, Synthesis, Molecular Docking Study and Anti-Hepatocellular Carcinoma Evaluation of Some New Bis-Triazolothiadiazines.
Abstract The reaction of bis(4-amino-4H-1,2,4-triazole-3-thiol) with hydrazonoyl halides and α-haloketones gave a new series of bis-1,2,4-triazolo[3,4-b]thiadiazine derivatives. The structure of the new products was established on the basis of their elemental and spectral data (mass, 1H NMR, 13C NMR and IR) and an alternate method. Several of the synthesized products were subjected to in vitro anticancer screening against human hepatocellular carcinoma (HepG-2) and the results showed that compounds 16, 14 and 12 have promising activities (IC50 value of 24.8±9.1, 28.3±0.5, and 31±2.9μM...
Source: Mini Reviews in Medicinal Chemistry - October 15, 2019 Category: Chemistry Authors: Gomha SM, Muhammad Z, Ezz-Elarab E, Elmetwally A, Matar I Tags: Mini Rev Med Chem Source Type: research

Synthesis and biological activity of hydrazones and derivatives: A review.
r JDF Abstract Hydrazones and their derivatives are very important compounds in medicinal chemistry due to their reported biological activity for the treatment of several diseases, like Alzheimer's, cancer, inflammation, and leishmaniasis. However, most of the investigations on hydrazones available in literature today, are directed to the synthesis of these molecules with little discussion available on their biological activities. With the purpose of bringing lights into this issue we performed a revision of the literature and wrote this review based on some of the most current research reports of hydrazones and d...
Source: Mini Reviews in Medicinal Chemistry - October 14, 2019 Category: Chemistry Authors: Carneiro Brum JO, França TCC, Villar JDF Tags: Mini Rev Med Chem Source Type: research

Quercetin-amino acid conjugates are promising anti-cancer agents in drug discovery projects.
Abstract Quercetin is a plant flavonoid with great potential for the prevention and treatment of disease. Despite the curative application of quercetin is hampered by low bioavailability, its core serves as a scaffold for generating more potent compounds with amplified therapeutic window. This review aims to describe recent advances in the improvement of the pharmacokinetic profile of quercetin via the amino acid prodrug approach which offers wide structural diversity, physicochemical and biological properties improvement. According to the findings, conjugation of quercetin with amino acids results in increased so...
Source: Mini Reviews in Medicinal Chemistry - October 9, 2019 Category: Chemistry Authors: Dobrydnev AV, Tkachuka TM, Atamaniuka VP, Popova MV Tags: Mini Rev Med Chem Source Type: research

A mini review on peptides as potential antifungal therapeutics.
Abstract Continuous increase in antimicrobial resistance and limited number of antifungal drugs forced us to search for new antifungal molecules with novel mechanism of action. Natural antimicrobial peptides, which are ubiquitous component of innate immunity, represent their candidature for novel antifungal peptides. Various antifungal peptides have been isolated from different species ranging from small marine organisms to insects and from various other living species. Based on these peptides various mimetic of antifungal peptides have also been synthesized using non-natural amino acids. Utilization of these anti...
Source: Mini Reviews in Medicinal Chemistry - September 26, 2019 Category: Chemistry Authors: Sharma D, Bisht GS Tags: Mini Rev Med Chem Source Type: research

Hypericum SPP.: An Update On The Biological Activities And Metabolic Profiles.
Abstract Plants from the genus Hypericum, one genera of the Hypericaceae family, have attracted a lot of attention for their potential pharmaceutical applications. Most of the studies in the literature focus on H. perforatum L. (common St. John's wort), whose complex spectrum of bioactive compounds makes this species one of the top herbal remedies and supplements in the world. It is also important to compare the studies of other Hypericum species, both from the phytochemical and from the biological point of view. The aim of this review is to provide an update of most recent studies about biological investigations ...
Source: Mini Reviews in Medicinal Chemistry - September 26, 2019 Category: Chemistry Authors: Marrelli M, Statti G, Conforti F Tags: Mini Rev Med Chem Source Type: research

Coumarin-based Scaffold as α-glucosidase Inhibitory Activity: Implication for Development of Potent Antidiabetic Agents.
Coumarin-based Scaffold as α-glucosidase Inhibitory Activity: Implication for Development of Potent Antidiabetic Agents. Mini Rev Med Chem. 2019 Sep 25;: Authors: Tafesse TB, Bule MH, Khoobi M, Faramarzi MA, Abdollahi M, Amini M Abstract Delaying the absorption of glucose through α-glucosidase enzymes inhibition is one of the therapeutic approaches in the management of Type 2 diabetes, which can reduce the incidence of postprandial hyperglycemia. The existence of chronic postprandial hyperglycemia impaired the endogenous antioxidant defense due to inducing oxidative stress induced pancreat...
Source: Mini Reviews in Medicinal Chemistry - September 25, 2019 Category: Chemistry Authors: Tafesse TB, Bule MH, Khoobi M, Faramarzi MA, Abdollahi M, Amini M Tags: Mini Rev Med Chem Source Type: research

First Synthesis for Bis-Spirothiazolidine Derivatives as a Novel Heterocyclic Framework and Their Biological Activity.
CONCLUSION: The novel bis-spirothiazolidine deriviatives synthesized for the first time and showed excellent anticancer activities. PMID: 31538895 [PubMed - as supplied by publisher] (Source: Mini Reviews in Medicinal Chemistry)
Source: Mini Reviews in Medicinal Chemistry - September 20, 2019 Category: Chemistry Authors: Flefel EM, Sofany WI, Awad HM, Shahat ME Tags: Mini Rev Med Chem Source Type: research

Dietary fatty acids-effects on cardiovascular disease.
Abstract Cardiovascular disease is a major cause of morbidity and mortality globally. There have been many studies on the relationship between the effects of dietary fatty acids and cardiovascular disease (CVD). These papers suggest that omega 3 may be protective against CVD. Saturated fatty acids and trans fatty acids have less benefits in health and remain associated with increased risk of CVD. However, the effects of omega 6 remains misunderstood. In this review, we aimed to evaluate the relation between different free fatty acids and the risk of cardiovascular disease based on recent experimental and clinical ...
Source: Mini Reviews in Medicinal Chemistry - September 19, 2019 Category: Chemistry Authors: Kh JK, Kh SK, Afshari A, Rezayi M, Ghayour-Mobarhan M Tags: Mini Rev Med Chem Source Type: research

Synthesis, and molecular docking stimulation of Novel bis-1,4-Dihydropyridines Linked to Aliphatic or Arene Core via Amide or Ester-Amide Linkages.
Abstract Novel bis(1,4-dihydropyridine-3,5-dicarbonitrile) derivatives linked to arene core via amide or ester-amide linkages were prepared and their structures were confirmed by several spectral tools. The synthesis of novel N,N'-(alkanediyl)bis(2-(2-(3,5-dicyano-2,6-dimethyl-1,4-dihydropyridin-4-yl)phenoxy)acetamide) by an acid-catalyzed condensation of the bis-aldehydes with four equivalents of 3-aminocrotononitrile was reported. The structures of the synthesized compounds were confirmed by the different spectral tools. The molecular docking stimulation studied indicated that, the prepared compounds are pr...
Source: Mini Reviews in Medicinal Chemistry - September 19, 2019 Category: Chemistry Authors: Abdella AM, Abdelmoniem AM, Ibrahim NS, El-Hallouty SM, Abdelhamid IA, Elwahy AHM Tags: Mini Rev Med Chem Source Type: research

Benzocaine: Review on a Drug with Unfold Potential.
Abstract Benzocaine has been well-known for its role as anesthetic agent and largely used in oral ulcers, ear pain and dental complications. Along with lidocaine and other local anesthetics, benzocaine has marked its part as an anesthetic in surgical procedures and as Na+ channels blocker, as well. Analogues of benzocaine have been found to possess biological potentials including antibacterial antifungal and anti-cancer. Some derivatives were found to have conspicuous action against tuberculosis. Current review focuses to explore the century long potential of the molecule and its analogs that have appeared in the ...
Source: Mini Reviews in Medicinal Chemistry - September 13, 2019 Category: Chemistry Authors: Khair-Ul-Bariyah S, Ali M, Din MI, Sharif A, Ahmed E, Arshad M Tags: Mini Rev Med Chem Source Type: research

New advances of heparanase in human diseases.
Abstract As we all know, heparanase plays an important role in human diseases. As a kind of endo-β-dglucuronidase, heparanase is the known only enzyme in mammals which could degrade heparan sulfate(HS) specifically. HS is a vital component of extracellular matrix(ECM). Heparanase takes effect by cleaving theβ(1,4)-glycosidic between glucosamine residue and glucuronic acid of HS. This cleavage will cause ECM remodelling and HS-linked biological molecules release, including cytokines, growth factors and a lot of biological molecules regulating various pathological activities. Experiments already proved tha...
Source: Mini Reviews in Medicinal Chemistry - September 13, 2019 Category: Chemistry Authors: Jin H, Cui M Tags: Mini Rev Med Chem Source Type: research

Natural polysaccharides with immunomodulatory activities.
Abstract Natural polysaccharides can be extracted from plants, fungi, algae, animals, and bacteria. The monosaccharide compositions and glucosidic bonds of polysaccharides from different origins vary substantially. Natural polysaccharides have been shown to possess a variety of biological activities including antitumor, anticoagulant, antioxidative, antiviral, immunomodulatory, antihyperlipidemic and antihepatotoxic activities. Their properties are mainly due to their structure characteristics. The present paper will review the mechanisms of the immunomodulatory activities of natural polysaccharides. In particular...
Source: Mini Reviews in Medicinal Chemistry - September 13, 2019 Category: Chemistry Authors: Zhao Y, Yan B, Wang Z, Li M, Zhao W Tags: Mini Rev Med Chem Source Type: research

Identification of Inhibitors against Botulinum Neurotoxins: 8-Hydroxyquinolines Hold Promise.
Abstract Botulinum neurotoxins (BoNTs) are the most toxic category A biological warfare agent. There is no therapeutics available for BoNT intoxication yet, necessitating the development of a medical countermeasure against these neurotoxins. The discovery of small molecule-based drugs has revolutionized in the last two decades resulting in the identification of several small molecule inhibitors of BoNTs. However, none progressed to clinical trials. 8-Hydroxyquinolines scaffold based molecules are important 'privileged structures' that can be exploited as inhibitors of a diverse range of targets. In this review, ou...
Source: Mini Reviews in Medicinal Chemistry - September 6, 2019 Category: Chemistry Authors: Chauhan R, Chauhan V, Sonkar P, Dhaked RK Tags: Mini Rev Med Chem Source Type: research

Hyaluronan Fragmentation During Inflammatory Pathologies: A Signal That Empowers Tissue Damage.
Abstract The mechanisms that modulate the response to tissue injury are not fully understood. Abnormalities in the repair response are associated with a variety of chronic disease states characterized by inflammation, followed subsequently by excessive extracellular matrix (ECM) deposition. As cell-matrix interactions is able to regulate cellular homeostasis, modification of ECM integrity appears to be an unspecific factor in promoting the onset and progression of inflammatory diseases. Evidence is emerging to show that endogenous ECM molecules supply signals to damaged tissues and cells in order to promote furthe...
Source: Mini Reviews in Medicinal Chemistry - September 6, 2019 Category: Chemistry Authors: Avenoso A, Bruschetta G, D Ascola A, Scuruchi M, Mandraffino G, Saitta A, Campo S, Campo GM Tags: Mini Rev Med Chem Source Type: research

Recent advances in application of azobenzenes grafted on Mesoporous Silica Nanoparticles in controlled Drug Delivery Systems using light as external stimulus.
ky AK Abstract Hybrid materials based in mesoporous silica nanoparticles (MSN) have attracted plentiful attention due to the versatility of their chemistry, and the field of drug delivery systems (DDS) is not an exception. MSN present a desirable biocompatibility, high surface area values, and a well-studied surface reactivity for tailoring a vast diversity of chemical moieties. Particularly important for DDS applications is using of external stimuli for drug release. In this context light is an exceptional alternative due to its high degree of spatiotemporal precision and non-invasive character, and large number ...
Source: Mini Reviews in Medicinal Chemistry - September 4, 2019 Category: Chemistry Authors: Ramírez-Rave S, Bernad-Bernad MJ, Gracia-Mora J, Yatsimirsky AK Tags: Mini Rev Med Chem Source Type: research

3D-QSAR and docking study of 2-((pyridin-3-yloxy)methyl) piperazines as α7 nicotinic acetylcholine receptor modulators for the treatment of inflammatory disorders.
3D-QSAR and docking study of 2-((pyridin-3-yloxy)methyl) piperazines as α7 nicotinic acetylcholine receptor modulators for the treatment of inflammatory disorders. Mini Rev Med Chem. 2019 Sep 04;: Authors: Purohit D, Saini V, Kumar S, Kumar A, Narasimhan B Abstract Comparative molecular field analysis (CoMFA) of 27 analogues of 2-((pyridin-3-yloxy)methyl)piperazine derivatives was carried out using software Tripos SYBYL X. Optimal r2 (0.854) and q2 (0.541) values were obtained for developed 3D QSAR model. The contour plots obtained from CoMFA analysis have shown 13.84% steric contribution and 66...
Source: Mini Reviews in Medicinal Chemistry - September 4, 2019 Category: Chemistry Authors: Purohit D, Saini V, Kumar S, Kumar A, Narasimhan B Tags: Mini Rev Med Chem Source Type: research

The therapeutic potential of miR-7 in cancers.
Abstract MiRNAs play an important role in the initiation and development of cancers. As a potent tumor suppressor, miRNA-7(miR-7) has been demonstrated to be significantly associated with the diverse fundamental biological processes in multiple cancer types including initiation, growth, metastasis and prognosis by targeting a number of molecules and signaling pathways. This current review summarizes and discusses the significance of the relationship between miR-7 and tumors. It may provide new integrative understanding for future studies on the exact role of miR-7 in cancers. PMID: 31483230 [PubMed - as suppl...
Source: Mini Reviews in Medicinal Chemistry - September 4, 2019 Category: Chemistry Authors: Li M, Pan M, You C, Dou J Tags: Mini Rev Med Chem Source Type: research

Rhodiola and salidroside in the treatment of metabolic disorders.
Abstract Over the past three decades, the knowledge gained about the mechanisms that underpin the potential use of Rhodiola in stress- and ageing-associated disorders has increased, and provided a universal framework for studies that focused on the use of Rhodiola in preventing or curing metabolic diseases. Of particular interest is the emerging role of Rhodiola in the maintenance of energy homeostasis. Moreover, over the last two decades, great efforts have been undertaken to unravel the underlying mechanisms of action of Rhodiola in the treatment of metabolic disorders. Extracts of Rhodiola and salidroside, the ...
Source: Mini Reviews in Medicinal Chemistry - September 3, 2019 Category: Chemistry Authors: Bai XL, Deng XP, Wu GJ, Li WJ, Jin S Tags: Mini Rev Med Chem Source Type: research

Ectonucleotidases: Potential Target in Drug Discovery and Development.
Abstract PMID: 31379303 [PubMed - in process] (Source: Mini Reviews in Medicinal Chemistry)
Source: Mini Reviews in Medicinal Chemistry - August 6, 2019 Category: Chemistry Authors: Iqbal J Tags: Mini Rev Med Chem Source Type: research

Soluble guanylate cyclase stimulators and activators: Where are we, where to go?
Abstract Soluble guanylate cyclase (sGC) is the intracellular receptor of messenger nitric oxide (NO). The activation of sGC results in the conversion of guanosine triphosphate (GTP) to the secondary messenger cyclic guanosine monophosphate (cGMP). cGMP modulates a series of cascades downstream through activating a variety of effectors, such as phosphodiesterase (PDE), protein kinase G (PKG), cyclic nucleotide gated ion channels (CNG). The NO-sGC-cGMP pathway play significant roles in various physiological processes, including platelet aggregation, smooth muscle relaxation and neurotransmitter delivery. Riociguat,...
Source: Mini Reviews in Medicinal Chemistry - July 30, 2019 Category: Chemistry Authors: Xiao S, Li Q, Hu L, Yu Z, Yang J, Chang Q, Chen Z, Hu G Tags: Mini Rev Med Chem Source Type: research

Natural Tyrosinase Inhibitors: Role of Herbals in the Treatment of Hyperpigmentary Disorders.
Abstract Cutaneous pigmentation plays critical role in determining the color of skin along with photo protection of skin from dreadful effects of ultraviolet radiations. Conversely, abnormal accumulation of melanin is responsible for hyper pigmentary disorders such as melasma, senile lentigines and freckles. Because of the visible nature of dermatologic diseases, they have a considerable psychosomatic effect on affected patients. Tyrosinase inhibitors are molecules that interrelate in some way with the enzyme to prevent it from working in the normal manner. Past many decades witnessed the quest for the development...
Source: Mini Reviews in Medicinal Chemistry - June 29, 2019 Category: Chemistry Authors: Zaidi KU, Ali SA, Ali A, Naaz I Tags: Mini Rev Med Chem Source Type: research

Latent tuberculosis infection (LTBI) and its potential targets: An investigation into dormant phase pathogens.
This study also includes current preclinical and clinical aspects of tubercular infections and new approaches in tubercular drug discovery. PMID: 31241015 [PubMed - as supplied by publisher] (Source: Mini Reviews in Medicinal Chemistry)
Source: Mini Reviews in Medicinal Chemistry - June 25, 2019 Category: Chemistry Authors: Gutti G, Arya K, Singh SK Tags: Mini Rev Med Chem Source Type: research

Protective effects of phenylpropanoids and phenylpropanoid-rich essential oils on the cardiovascular system.
CONCLUSION: A better understanding of the protective effects of phenylpropanoids on the cardiovascular system is presented, thus paving the way towards future research on plant-based therapies for CVDs. PMID: 31218957 [PubMed - as supplied by publisher] (Source: Mini Reviews in Medicinal Chemistry)
Source: Mini Reviews in Medicinal Chemistry - June 19, 2019 Category: Chemistry Authors: Silva JA, Zuzarte M, Marques C, Girão H, Salgueiro L Tags: Mini Rev Med Chem Source Type: research

Natural Terpenoids as Neuroinflammatory Inhibitors in LPS-stimulated BV-2 Microglia.
Abstract BACKGROUND: Neuroinflammation is a typical feature of many neurodegenerative diseases, including Alzheimer's disease and Parkinson's disease. Microglia, the resident immune cells of the brain, readily become activated in response to infection or injury. Uncontrolled and overactivated microglia can release pro-inflammatory and cytotoxic factors and are the major culprit in neuroinflammation. Hence, research into novel neuroinflammatory inhibitors is of paramount importance for the treatment of neurodegenerative diseases. Bacterial lipopolysaccharide, widely used in studies of brain inflammation, initiates ...
Source: Mini Reviews in Medicinal Chemistry - June 11, 2019 Category: Chemistry Authors: Xu Y, Wei H, Gao J Tags: Mini Rev Med Chem Source Type: research

Spinacia oleracea Linn Considered as one of the Most Perfect Foods: an Pharmacological and Phytochemical Review.
CONCLUSIONS: S. oleracea is an important edible plant also used for ethnomedical therapy of obesity, inflammation of lungs, lumbago, flatulence, and treatment of urinary calculi. Pharmacological and phytochemical studies of this plant including bioactives, which have been adequately studied, support its uses in the traditional medicines. Additionally, prospects and future trends of this plant are proposed. PMID: 31161986 [PubMed - as supplied by publisher] (Source: Mini Reviews in Medicinal Chemistry)
Source: Mini Reviews in Medicinal Chemistry - June 2, 2019 Category: Chemistry Authors: Gutierrez RMP, Velazquez EG, Carrera SPP Tags: Mini Rev Med Chem Source Type: research

PPAR Ligands Containing Stilbene Scaffold.
Abstract Peroxisome proliferator activated receptors (PPARs) are transcriptional factors belonging to the ligand-activated nuclear receptor superfamily. They are ubiquitously expressed throughout the body. So far, three major subtypes have been identified, PPAR, PPARand PPAR. They are crucial for lipid and glucose metabolism, and are also involved in the regulation of several types of tumors, inflammation, cardiovascular diseases and infertility. The importance of these transcription factors in physiology and pathophysiology has been largely investigated. Synthetic PPAR ligands are widely used...
Source: Mini Reviews in Medicinal Chemistry - June 2, 2019 Category: Chemistry Authors: Fantacuzzi M, De Filippis B, Amoroso R, Giampietro L Tags: Mini Rev Med Chem Source Type: research

Synthesis of Azoloquinazolines and substituted benzothiazepine as antimicrobial agents.
Abstract A direct and efficient approach for the synthesis of new series of fused quinazolines with triazole, thiazole, benzimidazole and tetrazole has been preceded via the reaction of quinazoline thione derivative with halogenated compounds or cyclocondensation of arylidene of quinazoline derivative with heterocyclic amines. Also, dibenzo[b,e][1,4]thiazepine derivatives was synthesized through the reaction of 2,6-bis-(2-chloro-benzylidene)-cyclohexanone with o-aminothiophenol. The structures of all new synthesized heterocyclic compounds were confirmed and discussed on the bases of spectral data. The utility of t...
Source: Mini Reviews in Medicinal Chemistry - June 2, 2019 Category: Chemistry Authors: Kassem AF, Alshehrei F, Abbas EMH, Farghaly TA Tags: Mini Rev Med Chem Source Type: research

Chemical Synthesis, Mechanism of Action and Anticancer Potential of Medicinally Important Thiazolidin-2,4-dione Derivatives: A Review.
Abstract Thiazolidin-2,4-dione (TZD) possessing an active methylene constitute an important chemical class of compounds for the development of new drugs. So, many scholars have synthesized these derivatives as target molecules and evaluated their biological potential. Currently, some of the TZDs are synthesized to treat human cancers stating high levels of PPARγ because it is expected that activation of PPARγ arbitrates their anticancer activity because PPARγ ligands have recently been established to affect differentiation, cell proliferation and apoptosis of different cell types. In the present ...
Source: Mini Reviews in Medicinal Chemistry - May 12, 2019 Category: Chemistry Authors: Kumar H, Deep A, Marwaha RK Tags: Mini Rev Med Chem Source Type: research

Bisphosphonates and cancer: A relationship beyond the antiresorptive effects.
In conclusion, BPs are considered the primary therapy for skeletal disorders due to its high affinity for bone, but now they are also considered as potential antitumor agents due to its ability to induce tumor cell apoptosis, inhibition of cell adhesion, invasion and proliferation, modulation of the immune system to target and eliminate cancer cells as well as affect the angiogenic mechanisms. Like any other drug, they also have some adverse effects, but the most common, the acute phase reaction, can be minimized with the intake of calcium and vitamin D. PMID: 31020940 [PubMed - as supplied by publisher] (Source: Mini...
Source: Mini Reviews in Medicinal Chemistry - April 24, 2019 Category: Chemistry Authors: Teixeira S, Branco LC, Fernandes MH, Costa-Rodrigues J Tags: Mini Rev Med Chem Source Type: research

2,4-Thiazolidinediones as PTP 1B Inhibitors: A Mini Review (2012-2018).
Abstract 2,4-thiazolidinedione (TZD) scaffold is a synthetic versatile scaffold explored by medicinal chemists for the discovery of novel molecules for the target-specific approach to treat or manage number of deadly ailments. PTP 1B is the negative regulator of insulin signaling cascade, and its diminished activity results in abolishment of insulin resistance associated with T2DM. The present review focused on the seven years journey (2012-2018) of TZDs as PTP 1B inhibitors with the insight into the amendments in the structural framework of TZD scaffold in order to optimize/design potential PTP 1B inhibitors. We ...
Source: Mini Reviews in Medicinal Chemistry - April 11, 2019 Category: Chemistry Authors: Verma SK, Yadav YS, Thareja S Tags: Mini Rev Med Chem Source Type: research

Recent advances in apoptosis: The role of hydrazones.
l;çükgüzel ŞG Abstract The process of programmed cell death in higher eukaryotes (apoptosis), is generally characterized by distinct morphological characteristics and energy-dependent biochemical mechanisms. Apoptosis is considered as a vital component of various processes including normal cell turnover, proper development and functioning of the immune system, hormone-dependent atrophy, embryonic development and chemical-induced cell death. Apoptosis seems to play an important key role in the progression of several human diseases like Alzheimer's disease, Parkinson's disease and many types of can...
Source: Mini Reviews in Medicinal Chemistry - April 10, 2019 Category: Chemistry Authors: Çıkla-Süzgün P, Küçükgüzel ŞG Tags: Mini Rev Med Chem Source Type: research

Chemistry, Analysis, Pharmacokinetics and Pharmacodynamics aspects of Lorcaserin, a selective serotonin 5-HT2C receptor agonist: An update.
Abstract This review refers to the all-inclusive details of Lorcaserin Hydrochloride, on comprehensive information about synthesis, analytical methods, pharmacodynamics, pharmacokinetics, drug interaction, and adverse effect. Lorcaserin Hydrochloride is (R)-8-Chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride chemically. Lorcaserin HCl is a novel synthetic, centrally acting selective serotonin C (5-HT2c) receptor, l agonist, which results in increased satiety and decreased food consumption in patients. A headache, dizziness, nausea, is the most common side effects associated with this drug. Lorcaser...
Source: Mini Reviews in Medicinal Chemistry - April 8, 2019 Category: Chemistry Authors: Sharma S, Aware KS, Hatware K, Patil K Tags: Mini Rev Med Chem Source Type: research

Passive, Active and Ultrasonic Drug Delivery.
Abstract Cancer has become one of the most deadly non-communicable diseases globally. Several modalities used to treat cancer patients exist today yet many have failed to prove high efficacy and low side effects. The most common example of such modalities is the use chemotherapeutic drugs to destroy cancerous cells and deter their uncontrolled proliferation. Parallel to the destruction of cancerous tissue; chemotherapy destroys normal, healthy tissues, as it lacks the specificity to annihilate cancerous cells preferentially resulting in adverse side effects that include nausea, hair fall, and cardiac infarction. T...
Source: Mini Reviews in Medicinal Chemistry - April 8, 2019 Category: Chemistry Authors: Basha SA, Dalibalta S, Husseini GA Tags: Mini Rev Med Chem Source Type: research

Exploring signaling pathways and pancreatic cancer treatment approaches using genetic models.
Abstract Despite available treatment options, the overall survival rates of pancreatic cancer patients remain dismal. Multiple counter-regulatory pathways have been identified and shown to be involved in interfering with the efficacy of therapeutic agents. In addition, various known genetic alterations in the cellular signaling pathways have been implicated in affecting the growth and progression of pancreatic cancer. Nevertheless, the significance of other unknown pathways is yet to be explored, which provides the rationale for the intervention of new approaches. Several experimental genetic models have been expl...
Source: Mini Reviews in Medicinal Chemistry - March 27, 2019 Category: Chemistry Authors: Khader S, Thyagarajan A, Sahu RP Tags: Mini Rev Med Chem Source Type: research

Protective Role of Natural Products in Cisplatin-Induced Nephrotoxicity.
Abstract Cisplatin is a widely used antineoplastic agent for the treatment of metastatic tumors, advanced bladder cancer and many other solid tumors. However, at higher doses, toxicities such as nephrotoxicity may appear. Cisplatin leads to DNA damage and subsequently renal cell death. Besides that, oxidative stress is also implicated as one of the main causes of nephrotoxicity. Several studies showed that numerous natural products: ginseng, curcumin, licorice, honey and pomegranate were able to reduce the oxidative stress by restoring the levels of antioxidant enzymes and also at the same time act as an anti-infl...
Source: Mini Reviews in Medicinal Chemistry - March 20, 2019 Category: Chemistry Authors: Ridzuan NRA, Rashid NA, Othman F, Budin SB, Hussan F, Teoh SL Tags: Mini Rev Med Chem Source Type: research

Detoxification of Heterocyclic Aromatic Amines by Probiotic to Inhibit Medical Hazards.
Abstract Cancer is the second leading factor of human death in the world. Long-term consumption of cooked red meat brings about various types of cancers like colorectal cancer due to formation of heterocyclic aromatic amines (HAAs) during the heating process of meat. There are various solutions for the reduction of these toxicants. The aim of this article is describing probiotic as one of possible strategies for bioremoval of these carcinogenic and mutagenic substances and changing food to functional one as well. The mechanism of mentioned biodetoxification is binding by probiotics, which depends on some variables...
Source: Mini Reviews in Medicinal Chemistry - March 17, 2019 Category: Chemistry Authors: Khosravi-Darani K, Barzegar F, Baghdadi M Tags: Mini Rev Med Chem Source Type: research

Malaria Hybrids: A Chronological Evolution.
Abstract Malaria, an upsetting malaise caused by diverse class of Plasmodium species effects about 40% of world population. The distress associated with it has reached colossal scales owing to the development of resistance to most of the clinically available agents. Hence, the search of newer molecules for malaria treatment and cure is an incessant process. After the era of single molecule for malaria treatment ended, there was an advent of combination therapy. However, lately there have been reports of development of resistance to many of these agents as well. Subsequently, at present most of the peer group worki...
Source: Mini Reviews in Medicinal Chemistry - March 14, 2019 Category: Chemistry Authors: Marella A, Verma G, Shaquiquzzaman M, Khan MF, Akhtar W, Alam MM Tags: Mini Rev Med Chem Source Type: research

Brain-eating amoebae infection: challenges and opportunities in chemotherapy.
Abstract Pathogenic free-living amoeba are known to cause devastating infection of the central nervous system and are often referred to as "brain-eating amoebae". The mortality rate of more than 90% and free-living nature of these amoebae is a cause for concern. It is distressing that the mortality rate has remained the same over the past few decades highlighting lack of interest by the pharmaceutical industry. With the threat of global warming and increased outdoor activities of public, there is a need for renewed interest in identifying potential anti-amoebic compounds for successful prognosis. Here, w...
Source: Mini Reviews in Medicinal Chemistry - March 13, 2019 Category: Chemistry Authors: Mungroo MR, Anwar A, Khan NA, Siddiqui R Tags: Mini Rev Med Chem Source Type: research

Exploring the chemistry and therapeutic potential of triazoles: A comprehensive literature review.
The objective of the review is to endow with the insights to not only the synthetic but also to the medicinal chemists so as to design and synthesize the novel triazole derivatives with advanced and unexplored pharmacological implications. PMID: 30864516 [PubMed - as supplied by publisher] (Source: Mini Reviews in Medicinal Chemistry)
Source: Mini Reviews in Medicinal Chemistry - March 12, 2019 Category: Chemistry Authors: Jain A, Piplani P Tags: Mini Rev Med Chem Source Type: research

Potentials of Diphenyl Ether Scaffold as a Therapeutic Agent: A Review.
Abstract Diphenyl ethers (DPE) and its analogs have exhibited an excellent potential for therapeutic and industrial applications. Since the 19th century, intensive research is perpetuating on the synthetic routes and biological properties of DPEs. Few well-known DPEs are Nimesulide, Fenclofenac, Triclosan, Sorafenib, MK-4965, and MK-1439 which have shown the potential of this moiety as a lead scaffold for different pharmacological properties. In this review, we recapitulate the diverse synthetic route of DPE moiety inclusive of merits and demerits over the classical synthetic route and how this moiety sparked an i...
Source: Mini Reviews in Medicinal Chemistry - March 12, 2019 Category: Chemistry Authors: Kini SG, Rathi E, Kumar A, Bhat V Tags: Mini Rev Med Chem Source Type: research

Antidotes against methanol poisoning, a review.
Abstract methanol is the simplest alcohol at all. Comparing to ethanol that is fully detoxified by metabolism, methanol become activated to toxic products by enzymes alcohol dehydrogenase and aldehyde dehydrogenase. Paradoxically, the same enzymes convert ethanol up to harmless acetic acid. This review is focused on discussion and overview of literature devoted to methanol toxicology and antidotal therapy. Regarding to the antidotal therapy, three main approaches are presented in the text: 1) ethanol as a competitive inhibitor on alcohol dehydrogenase; 2) use of drugs like fomepizole inhibiting alcohol dehydrogena...
Source: Mini Reviews in Medicinal Chemistry - March 12, 2019 Category: Chemistry Authors: Pohanka M Tags: Mini Rev Med Chem Source Type: research

A Review on the Antitumor Activity of Various Nitrogenous-based Heterocyclic Compounds as NSCLC Inhibitors.
Abstract At present, cancers have been causing deadly fears to humans and previously incogitable losses to health. Especially, lung cancer is one of the most common causes of cancer-related mortality accounting for approximately 15% of all cancer cases worldwide. While non-small cell lung carcinomas (NSCLCs) makes up to 80% of lung cancer cases. The patient compliance has been weakening because of serious drug resistance and adverse drug effects. Therefore there is an urgent need for the development of novel structural agents to inhibit NSCLCs. Nitrogen-containing heterocyclic compounds exhibit wide range of biolo...
Source: Mini Reviews in Medicinal Chemistry - March 12, 2019 Category: Chemistry Authors: Liu JC, Narva S, Zhou K, Zhang W Tags: Mini Rev Med Chem Source Type: research

Follistatin-like 1 in Cardiovascular Disease and Inflammation.
Abstract Follistatin-like 1 (FSTL1), a secreted glycoprotein, has been shown to participate in regulating developmental processes and to be involved in states of disease and injury. Spatiotemporal regulation and posttranslational modifications contribute to its specific functions and make it an intriguing candidate to study disease mechanisms and potentially develop new therapies. With cardiovascular diseases as the primary cause of death worldwide, clarification of mechanisms underlying cardiac regeneration and revascularization remains essential. Recent findings on FSTL1 in both acute coronary syndrome and heart...
Source: Mini Reviews in Medicinal Chemistry - March 12, 2019 Category: Chemistry Authors: Peters MMC, Meijs TA, Gathier W, Doevendans PAM, Sluijter JPG, Chamuleau SAJ, Neef K Tags: Mini Rev Med Chem Source Type: research

Therapeutic Potential of Vanillin and its Main Metabolites to Regulate the Inflammatory Response and Oxidative Stress.
Abstract Many phenolic compounds found in foods and medicinal plants have shown interesting therapeutic potential and have attracted the attention of the pharmaceutical industry as promising pharmacologically active compounds in health promotion and disease prevention. Vanillin is a phenolic aldehyde, widely used as a flavoring agent in the food, pharmaceutical, and cosmetics industries. A variety of pharmacological activities has been attributed to this compound and its main metabolites, vanillic acid and vanillyl alcohol, including their anti-inflammatory ability. The relationship of the anti-inflammatory effect...
Source: Mini Reviews in Medicinal Chemistry - March 12, 2019 Category: Chemistry Authors: Bezerra-Filho CSM, Barboza JN, Souza MTS, Sabry P, Ismail NSM, de Sousa DP Tags: Mini Rev Med Chem Source Type: research

Synthesis, Docking Studies into CDK-2 and Anticancer Activity of New Derivatives Based Pyrimidine Scaffold and Their Derived Glycosides.
Abstract New diaryl-substituted pyrimidinedione compounds, their thioxo derivatives as well as their bicyclic thiazole compounds were synthesized and characterized. The glycosylamino derivatives of the synthesized disubstituted derivatives of the pyrimidine scaffold were also prepared via reaction of the N3-amino derivatives with a number of monosaccharides followed by acetylation. The anticancer activity of the synthesized compounds was studied against human liver cancer (HepG2) and RPE-1cell lines. Compounds 2a, 2b, 3a and 12 showed potent activities with IC50 results comparable to that of doxorubicin. Docking i...
Source: Mini Reviews in Medicinal Chemistry - March 12, 2019 Category: Chemistry Authors: Rahman AAHA, Nassar IF, Shaban AKF, El-Kady DS, Awad HM, El Sayed WA Tags: Mini Rev Med Chem Source Type: research

Recent Advances towards Treatment of HIV: Synthesis and SAR Studies.
This article has shelters and highpoints the recent advancement of innumerable inhibitors laterally through synthetic, semi-synthetic and structure activity relationship (SAR) approaches. PMID: 30864523 [PubMed - as supplied by publisher] (Source: Mini Reviews in Medicinal Chemistry)
Source: Mini Reviews in Medicinal Chemistry - March 12, 2019 Category: Chemistry Authors: Shrivastava N, Husain A, Rashid M, Karim S, Alsabeelah NF, Siddiqui NA Tags: Mini Rev Med Chem Source Type: research

Pharmacological aspects and potential use of phloretin: a systemic review.
Abstract Over the past two decades, many researchers have concluded that a diet rich in polyphenolic compounds plays an important therapeutic role in reducing the risk of cancer, cardiovascular disease, inflammation, type II diabetes, and other degenerative diseases. Polyphenolic compounds have been reported to be involved in neutralization of reactive oxygen species and charged radicals, and have anti-carcinogenic effects, hepatoprotective effects, low-glycaemic response, and other benefits. The benefits of fruits and vegetables may be partly attributable to polyphenolic compounds, which have antioxidant and free...
Source: Mini Reviews in Medicinal Chemistry - March 11, 2019 Category: Chemistry Authors: Mariadoss AVA, Vinyagam R, Rajamanickam V, Senthilkumar V, Venkatesan S, David E Tags: Mini Rev Med Chem Source Type: research

Analysis of the essential oils of five Artemisia species and evaluation of their cytotoxic and proapoptotic effects.
In this study, the essential oil composition and cytotoxic activities of five Artemisia species was determined. The collected plants were water-distilled separately to obtain oils which were subjected to GC and GC/MS in order to identify their compositions. The cancer cells were exposed to different concentrations of samples. The cell viability was measured by AlamarBlue® assay. The apoptotic cells were analyzed by PI staining and Flow Cytometry. To study the amount of pro-apoptotic proteins and the apoptosis mechanism, the western blot method was used. The number of compounds in the oils was determined. Although all s...
Source: Mini Reviews in Medicinal Chemistry - March 11, 2019 Category: Chemistry Authors: Tayarani-Najaran Z, Akaberi M, Hassanzadeh B, Shirazi N, Asili J, Al-Najjar H, Sahebkar A, Emami SA Tags: Mini Rev Med Chem Source Type: research

Pathological role of advanced glycation end products (AGEs) and their receptor axis in atrial fibrillation.
Abstract Accumulating evidence has shown that incidence of atrial fibrillation (AF) is higher in patients with diabetes, especially those with poor glycemic control or long disease duration. Non-enzymatic glycation of amino acids of proteins, lipids, and nucleic acids has progressed under normal aging process and/or diabetic condition, which could lead to the formation and accumulation of advanced glycation end products (AGEs). AGEs not only alter the tertiary structure and physiological function of macromolecules, but also evoke inflammatory and fibrotic reactions through the interaction of cell surface receptor ...
Source: Mini Reviews in Medicinal Chemistry - March 11, 2019 Category: Chemistry Authors: Yamagishi SI, Sotokawauchi A, Matsui T Tags: Mini Rev Med Chem Source Type: research