One-pot synthesis and in vitro bioactivity of novel 4-aminopyrazolo[3,4-b]pyridine derivatives as potential antimicrobial compounds
AbstractThe present paper describes an efficient synthesis of a series of 4-aminopyrazolo[3,4-b]pyridine derivatives11a –i in 69 –81% yields by one-pot three-component domino reaction of phenylhydrazine and two differentβ-ketonitriles in DMSO. All the synthesized derivatives were screened in vitro for their antimicrobial potential against seven Gram-positive and Gram-negative clinical bacterial strains and one fungal strain. Most of the tested derivatives displayed promising antimicrobial potency and activity was found to be comparable to standard drugs (amoxicillin and fluconazole). Compounds11a and11d with the MIC v...
Source: Medicinal Chemistry Research - November 23, 2023 Category: Chemistry Source Type: research
Kaempferia diterpenoids and flavonoids: an overview on phytochemistry, biosynthesis, synthesis, pharmacology, and pharmacokinetics
AbstractKaempferia species have contained various crucial ethnobotanical features, and are being used as traditional folk medicines in some Southeast Asia. This review tends to highlight important information (phytochemistry, biosynthesis, synthesis, pharmacology, and pharmacokinetics) ofKaempferia principal phytochemical classes diterpenoids and flavonoids. The electronic sources, e.g., Google Scholar, Sci-Finder, and Web of Science, and the most meaningful keywords “Kaempferia”, “diterpenoids”, and “flavonoids” have been more often utilized for searching the literature. More than 190 phytochemicals type diter...
Source: Medicinal Chemistry Research - November 21, 2023 Category: Chemistry Source Type: research
Design and synthesis of novel cycloalkanecarboxamide parabanic acid hybrids as anticonvulsants
AbstractAiming to develop novel anticonvulsant agents a new series of novel cycloalkanecarboxamide parabanic acid hybrids series8,9 and10 possessing the essential structure requirements for anticonvulsant activity was synthesized starting from cycloalkanones. All final target compounds were primary screened for chemically and electrically induced seizures using pentylenetetrazole “scPTZ” and maximal electroshock seizure “MES” models. In phase I anticonvulsant evaluation compounds8b and10b exhibited the highest potency among all the target compounds with 100% protection towards chemically induced seizures. Results o...
Source: Medicinal Chemistry Research - November 15, 2023 Category: Chemistry Source Type: research
Design, synthesis and antimicrobial activities of 1,2,3-triazole hybrids with amine-ester functionality
AbstractDue to the notable therapeutic importance of 1,4-disubstituted-1,2,3-triazoles linked with amine and ester groups, a series of 1,2,3-triazole hybrid containing amine-ester functionality have been synthesized. This synthesis involves a Cu(I) catalyzed [3 + 2] dipolar cycloaddition between N-substituted(prop-2-yn-1-yl)amines (3a –3d) and benzyl 2-azidoacetates (6a –6e). The triazoles were thoroughly characterized using different spectral techniques. In vitro assay of developed synthetics with different microbial strains includingS. aureus, B. Subtilis, E. Coli, S. enterica, C albicans andR. Oryzae have been ...
Source: Medicinal Chemistry Research - November 4, 2023 Category: Chemistry Source Type: research
Design, synthesis, and in silico studies of novel di-(2-aryl hydrozonopropanal) arene derivatives as potent anticancer for targeting A2AR and LRP6 in HCT116 cell
This study aimed to design and synthesize novel anticancer drug candidates and then examine their anticancer activity against human cancer cell lines. The anti-proliferation of human colon cancer cells (HCT116) was examined using the MMT assay and compared to the activity of doxorubicin as chemotherapy after characterizing novel derivatives of di (2-aryl hydrazonopropane) arene by elemental analyzer, FTIR, 1H, 13C NMR, and ESI-MS. Chemoinformatic tools predicted their targets, and then molecular docking was performed to predict the binding affinity of compounds to the main receptors expressed in colon cancer: the adenosine...
Source: Medicinal Chemistry Research - November 3, 2023 Category: Chemistry Source Type: research
Discovery of potent maternal embryonic leucine zipper kinase (MELK) inhibitors of novel chemotypes using structure-based pharmacophores
This study highlights the use of X-ray crystallographic structures t o boost the drug discovery process. (Source: Medicinal Chemistry Research)
Source: Medicinal Chemistry Research - October 28, 2023 Category: Chemistry Source Type: research
Screening of small molecule compounds targeting hnRNPA2 protein
In this study, a variety of small molecule compounds that can interact with A2 protein were screened from natural and synthetic compounds libraries using computer virtual screening technology and BIAcore high-throughput screening system. In many ways, such as isothermal tiorimetry calorimetry, fluorescence quenching assay, molecular docking simulation and cellular thermal shift assay, we confirmed the interactions between small molecule compounds EpimedinA1, G38 and hnRNPA2 proteins, respectively. Cell experiments showed that G38 inhibited the proliferation of MCF-7 cells and MDA-MB-231 cells in a dose-dependent manner. Fu...
Source: Medicinal Chemistry Research - October 28, 2023 Category: Chemistry Source Type: research
Correction: Structural and stereochemical determinants for hGAT3 inhibition: development of novel conformationally constrained and substituted analogs of (S)-isoserine
(Source: Medicinal Chemistry Research)
Source: Medicinal Chemistry Research - October 26, 2023 Category: Chemistry Source Type: research
Novel aloe emodin –hydroxyethyl piperazine hybrid dihydrochloride induces oral cancer CAL-27 cells apoptosis through ROS production, DNA damage and mitochondrial pathways
This study provides new insights into the further development of anthraquinone compounds as potential chemotherapeutic agents for oral cancer treatment.The novel aloe emodin derivativeAE-NPC induces oral cancer CAL-27 cells apoptosis through ROS production, DNA damage and mitochondrial pathways. The anthraquinone compoundAE-NPC may be a potential agent for the treatment of oral cancer. (Source: Medicinal Chemistry Research)
Source: Medicinal Chemistry Research - October 19, 2023 Category: Chemistry Source Type: research
The trimethoxyphenyl (TMP) functional group: a versatile pharmacophore
AbstractThe Trimethoxyphenyl (TMP) group serves as a pharmacophore in numerous potent agents exhibiting diverse bioactivity effects. This moiety is prominently present in the molecular structures of various research studies, demonstrating remarkable multi-activity or specific targeting, surpassing the activity of other derivatives at comparable concentrations. The compounds containing the TMP group have displayed notable anti-cancer effects by effectively inhibiting tubulin, heat shock protein 90 (Hsp90), thioredoxin reductase (TrxR), histone lysine-specific demethylase 1 (HLSD1), activin receptor-like kinase-2 (ALK2), P-g...
Source: Medicinal Chemistry Research - October 16, 2023 Category: Chemistry Source Type: research
Synthesis of 6,6-Dimethyl-3-azabicyclo [3.1.0]hexane via Ru (II)-catalyzed intramolecular cyclopropanation
Abstract6,6-Dimethyl-3-azabicyclo[3.1.0]hexane (6,6-DMABH) is a crucial component in several antiviral medications, such as boceprevir and pf-07321332. To enable more efficient synthesis of 6,6-DMABH, we have developed an innovative approach that utilizes intramolecular cyclopropanation of alpha-diazoacetatesvia Ru (II) catalysis and the Gabriel synthesis. Gram-scale synthesis of 6,6-DMABH from 3-methyl-2-butenol is achieved in seven distinct steps, resulting in a total yield of 28%. (Source: Medicinal Chemistry Research)
Source: Medicinal Chemistry Research - October 14, 2023 Category: Chemistry Source Type: research
1,2,3-triazole derivatives as antiviral agents
AbstractIn the last years, the emergence and spread of viral infections have been described with increased frequency and becomes a serious problem. The development of novel effective antiviral agents is urgently needed. 1,2,3-triazoles have attracted a big interest in medicinal chemistry for their various biological activities and diverse properties. This review aims to outline the advances in the application of 1,2,3-triazole derivatives as antiviral agents. (Source: Medicinal Chemistry Research)
Source: Medicinal Chemistry Research - October 9, 2023 Category: Chemistry Source Type: research
Evaluation of chemical constituents of Rooibos (Aspalathus linearis) and Honeybush (Cyclopia intermedia) as adenosine A1/A2A receptor ligands
AbstractRooibos (Aspalathus linearis) and Honeybush (Cyclopia intermedia) are popular tisanes in South Africa and are of growing interest due to the wide variety of flavonoids and other phytochemicals they contain. Despite their history as herbal teas and traditional medicines, the chemical constituents of these tisanes have yet to be studied for their effects on adenosine receptors. A series of 30 commercially available chemical constituents of Rooibos and Honeybush were investigated via radioligand binding studies to determine their adenosine A1 and A2A receptor affinity at both rat and human subtypes in order to establi...
Source: Medicinal Chemistry Research - October 5, 2023 Category: Chemistry Source Type: research
Current progress toward synthetic routes and medicinal significance of quinoline
AbstractQuinoline motifs are essential in several pharmacological active heterocyclic compounds due to their various applications in medicinal and industrial chemistry. Furthermore, there are greater societal expectations in the current scenario that synthetic and medicinal chemists should produce greener and more sustainable chemical processes. Therefore, this mini-review article highlights the traditional and green synthetic approaches of quinoline and its analogs, including multicomponent one-pot reactions and solvent-free reaction conditions utilizing microwave and ultraviolet irradiation-promoted synthesis using eco-f...
Source: Medicinal Chemistry Research - September 28, 2023 Category: Chemistry Source Type: research
Advances in research of ursolic acid and its derivatives as potential drug candidates against various types of lung cancers
AbstractAs one of the most common mortal diseases, the development of anti-lung cancer drugs is never stopped. Ursolic acid (UA) is a pentacyclic triterpenoid with significant anti-lung cancer activity and low toxicity. The bottleneck of UA in clinical application is poor water solubility and bioavailability. Until now, many novel UA derivatives have been developed to overtake these problems. In this paper, the relationship between the structure and activity of different functional groups was discussed. All anti-lung cancer ursolic acid derivatives were reviewed, and their biological activity and structure –activity rela...
Source: Medicinal Chemistry Research - September 25, 2023 Category: Chemistry Source Type: research
