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Novel coumarin linked pyrazoles, thiazoles, and thiadiazoles: synthetic strategies and in vitro antimicrobial investigation.

作者信息

Elsharabasy Salwa A, Sayed Mariam T, Abdel-Aziem Anhar

机构信息

Chemistry Department, Faculty of science(Girls), Al-Azhar University, Nasr City, Cairo, Egypt.

出版信息

Future Med Chem. 2025 Jan;17(2):183-193. doi: 10.1080/17568919.2024.2444867. Epub 2024 Dec 26.


DOI:10.1080/17568919.2024.2444867
PMID:39723730
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11749368/
Abstract

AIM: Emerging resistance among pathogens necessitates the development of novel antimicrobial agents. As a result, we aimed to synthesize new coumarins and study their antimicrobial activity with the hope of obtaining effective drugs. METHOD: A series of coumarins were synthesized, characterized, and assessed for antimicrobial activity using broth microdilution and agar diffusion methods against Gram-positive (), Gram-negative () bacteria, and fungi (). RESULTS: Pyrazoles and revealed promising activities against all bacterial strains with MIC values ranging from 1.95 to 15.6 µg/ml. Notably, pyrazole with CF in 3-position of pyrazole ring demonstrated higher ability to inhibit strain with MIC value equal to penicillin G (3.91 µg/ml). It also exhibited the best bactericidal potency against with MBC value of 15.6 µg/ml while, pyrazole recorded the same MBC value against . Pyrazole demonstrated the strongest antifungal activity against both fungal strains with MIC and MFC values of 15.6, 7.81, 62.5, and 31.3 µg/ml against and , respectively. CONCLUSION: These findings underscore the potential of coumarins, particularly compounds and , as effective antimicrobial agents and provide critical insights into the design of bioactive molecules.

摘要

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本文引用的文献

[1]
Synthesis and antimicrobial activity of new series of thiazoles, pyridines and pyrazoles based on coumarin moiety.

Sci Rep. 2023-6-19

[2]
Enzymatic Synthesis of a Novel Coumarin Aminophosphonates: Antibacterial Effects and Oxidative Stress Modulation on Selected Strains.

Int J Mol Sci. 2023-4-20

[3]
Synthesis and Biological Evaluation of Piperazine Hybridized Coumarin Indolylcyanoenones with Antibacterial Potential.

Molecules. 2023-3-9

[4]
Antibiotic combinations reduce Staphylococcus aureus clearance.

Nature. 2022-10

[5]
Molecular Insights into Coumarin Analogues as Antimicrobial Agents: Recent Developments in Drug Discovery.

Antibiotics (Basel). 2022-4-24

[6]
Coumarin thiazoles as unique structural skeleton of potential antimicrobial agents.

Bioorg Chem. 2022-7

[7]
Synthetic and natural coumarins as potent anticonvulsant agents: A review with structure-activity relationship.

J Clin Pharm Ther. 2022-7

[8]
Effect of methylpyrazoles and coumarin association on the growth of Gram-negative bacteria.

Arch Microbiol. 2022-2-3

[9]
Isolation, chemical characterization, and anti-inflammatory activity of coumarins, flavonoids, and terpenes from .

Nat Prod Res. 2022-9

[10]
Novel carbazole-oxadiazoles as potential Staphylococcus aureus germicides.

Pestic Biochem Physiol. 2021-6

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