Mrugesh J. Patel

Bio: Mrugesh J. Patel is an academic researcher from Charotar University of Science and Technology. The author has contributed to research in topics: Chemistry & Antibacterial activity. The author has an hindex of 2, co-authored 5 publications receiving 12 citations.

Coumarin–carbazole based functionalized pyrazolines: synthesis, characterization, anticancer investigation and molecular docking

Abstract: A series of novel pyrazoline scaffolds from coumarin–carbazole chalcones were synthesized. We explored various acetyl, amide, and phenyl substituents at the N-1 position of the pyrazoline core. The synthesized compounds were characterized by FTIR, 1H-NMR, 13C-NMR, DEPT, and mass spectroscopic techniques. The in vitro cytotoxicity study of all the synthesized compounds was evaluated against HeLa, NCI-H520 and NRK-52E cell lines. Compounds 4a and 7b became the most active compounds and exhibited their potential to arrest the cell cycle progression and induce apoptosis in both the cell lines. In addition, molecular docking studies revealed a higher binding affinity of both the molecules with CDK2 protein. Based on the obtained results, a comprehensive analysis is warranted to establish the role of compounds 4a and 7b as promising cancer therapeutic agents.

Design, synthesis, and characterization of novel substituted 1,2,4-oxadiazole and their biological broadcast

Abstract: In the current study, a novel combinatorial library of substituted 1,2,4-oxadiazoles bearing pyridine and thiazole have been synthesized via the condensation reaction of amidoxime and carboxylic acids and its derivatives in two way. The titled compounds were screened for their in vitro antimicrobial activity against three gram positive bacteria and three gram negative bacteria, In vitro antituberculosis activity against Mycobacterium tuberculosis H37RV and in vitro antimalarial activity against Plasmodium falciparum. Majority of the compounds were found to be active against gram positive bacteria. Compounds 6e, 6f, 7e, and 7f elaborate moderate antituberculosis activity against the first-line drug while 6c, 6d, 7c, and 7d intricate excellent antimalarial activity against Plasmodium falciparum strain.

Naphthalene substituted benzo[c]coumarins: Synthesis, characterization and evaluation of antibacterial activity and cytotoxicity

Abstract: Abstract Novel congeners of naphthalene substituted benzo[c]coumarins (2a-f) were synthesized by reaction of various 3-coumarinoyl methyl pyridinium bromide salts (1a-d) with a selected set of acetyl naphthalene in the presence of sodium acetate in refluxing glacial acetic acid. Structures of the synthesized compounds were confirmed by elemental analysis and by various spectroscopic techniques such as 1H-NMR, 13C-NMR, DEPT, and MS spectral data. Synthesised compounds were screened for antibacterial activity and cytotoxicity against different human cancer cell lines including cervix cancer (HeLa), breast cancer (MCF-7) and lung cancer (A549) using tetrazolium dye 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cell viability assay. Although with varying degrees, a significant growth inhibitory and cytotoxic effects were observed on all three cancer cell lines. Compounds 2b and 2e showed significant growth inhibitory and cytotoxicity against aforementioned cancer cell lines.

Metal free approach for One-pot synthesis of 3-aryl-furo[3,2-c]coumarins

Abstract: Various 3-aryl-furo[3,2-c]coumarins have been synthesized by reacting various 4-hydroxycoumarins with appropriate bromo-acetyl derivatives of furan, naphthalene and benzofuran under metal-free reaction condition. The effects of substitution, reaction temperature and reaction time for product formation were investigated. All the synthesized compounds were characterized by IR, H NMR, C NMR, DEPT-90, Mass spectral and elemental analysis.

Recent advances on anticancer activity of coumarin derivatives

Abstract: Coumarin derivatives are important class of natural plant metabolites that offer variety of biological activities. They can also be derived synthetically, and a wide variety of synthetic coumarin derivatives (azoles, sulfonyl, furan, pyrazole etc) have shown promising anticancer, antitumor and anti-proliferative activities. Coumarin derivatives are not only effective anticancer agents, but also possess minimum side effects. On the basis of different substitution patterns, these potents have displayed tremendous capability to regulate the potential anticancer activities. In view of the above, efforts have been made by the scientists to develop its scaffolds that possess minimal side effects. This review article covers the recent developments of coumarin derivatives that are biologically active against various cancer cell lines. Further, it also highlights the evaluation of these active candidates via in vivo, in vitro, MTT assay. The ongoing developments in the discovery of novel anti-cancer agents and their effectiveness using Structural Activity Relationship is also discussed in detail.

A Review of the Recent Development in the Synthesis and Biological Evaluations of Pyrazole Derivatives

Abstract: Pyrazoles are five-membered heterocyclic compounds that contain nitrogen. They are an important class of compounds for drug development; thus, they have attracted much attention. In the meantime, pyrazole derivatives have been synthesized as target structures and have demonstrated numerous biological activities such as antituberculosis, antimicrobial, antifungal, and anti-inflammatory. This review summarizes the results of published research on pyrazole derivatives synthesis and biological activities. The published research works on pyrazole derivatives synthesis and biological activities between January 2018 and December 2021 were retrieved from the Scopus database and reviewed accordingly.

Recent Applications of the Multicomponent Synthesis for Bioactive Pyrazole Derivatives

Abstract: Pyrazole and its derivatives are considered a privileged N-heterocycle with immense therapeutic potential. Over the last few decades, the pot, atom, and step economy (PASE) synthesis of pyrazole derivatives by multicomponent reactions (MCRs) has gained increasing popularity in pharmaceutical and medicinal chemistry. The present review summarizes the recent developments of multicomponent reactions for the synthesis of biologically active molecules containing the pyrazole moiety. Particularly, it covers the articles published from 2015 to date related to antibacterial, anticancer, antifungal, antioxidant, α-glucosidase and α-amylase inhibitory, anti-inflammatory, antimycobacterial, antimalarial, and miscellaneous activities of pyrazole derivatives obtained exclusively via an MCR. The reported analytical and activity data, plausible synthetic mechanisms, and molecular docking simulations are organized in concise tables, schemes, and figures to facilitate comparison and underscore the key points of this review. We hope that this review will be helpful in the quest for developing more biologically active molecules and marketed drugs containing the pyrazole moiety.

Coumarin–carbazole based functionalized pyrazolines: synthesis, characterization, anticancer investigation and molecular docking

Abstract: A series of novel pyrazoline scaffolds from coumarin–carbazole chalcones were synthesized. We explored various acetyl, amide, and phenyl substituents at the N-1 position of the pyrazoline core. The synthesized compounds were characterized by FTIR, 1H-NMR, 13C-NMR, DEPT, and mass spectroscopic techniques. The in vitro cytotoxicity study of all the synthesized compounds was evaluated against HeLa, NCI-H520 and NRK-52E cell lines. Compounds 4a and 7b became the most active compounds and exhibited their potential to arrest the cell cycle progression and induce apoptosis in both the cell lines. In addition, molecular docking studies revealed a higher binding affinity of both the molecules with CDK2 protein. Based on the obtained results, a comprehensive analysis is warranted to establish the role of compounds 4a and 7b as promising cancer therapeutic agents.

In vitro anti-TB properties, in silico target validation, molecular docking and dynamics studies of substituted 1,2,4-oxadiazole analogues against Mycobacterium tuberculosis.

Abstract: The alarming increase in multi- and extensively drug-resistant (MDR and XDR) strains of Mycobacterium tuberculosis (MTB) has triggered the scientific community to search for novel, effective, and safer therapeutics. To this end, a series of 3,5-disubstituted-1,2,4-oxadiazole derivatives (3a-3i) were tested against H37Rv, MDR and XDR strains of MTB. Of which, compound 3a with para-trifluorophenyl substituted oxadiazole showed excellent activity against the susceptible H37Rv and MDR-MTB strain with a MIC values of 8 and 16 µg/ml, respectively.To understand the mechanism of action of these compounds (3a-3i) and identify their putative drug target, molecular docking and dynamics studies were employed against a panel of 20 mycobacterial enzymes reported to be essential for mycobacterial growth and survival. These computational studies revealed polyketide synthase (Pks13) enzyme as the putative target. Moreover, in silico ADMET predictions showed satisfactory properties for these compounds, collectively, making them, particularly compound 3a, promising leads worthy of further optimisation.