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新型香豆素连接的吡唑、噻唑和噻二唑:合成策略及体外抗菌研究

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.

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

目的

病原体中不断出现的耐药性使得开发新型抗菌药物成为必要。因此,我们旨在合成新的香豆素并研究其抗菌活性,以期获得有效的药物。

方法

合成了一系列香豆素,对其进行了表征,并采用肉汤微量稀释法和琼脂扩散法针对革兰氏阳性()、革兰氏阴性()细菌及真菌()评估了抗菌活性。

结果

吡唑 和 对所有细菌菌株均显示出有前景的活性,其最小抑菌浓度(MIC)值范围为1.95至15.6微克/毫升。值得注意的是,吡唑环3位带有CF的吡唑 对 菌株的抑制能力更强,其MIC值与青霉素G相同(3.91微克/毫升)。它对 的杀菌效力也最佳,MBC值为15.6微克/毫升,而吡唑 对 的MBC值与之相同。吡唑 对两种真菌菌株均表现出最强的抗真菌活性,对 和 的MIC及MFC值分别为15.6、7.81, 62.5和31.3微克/毫升。

结论

这些发现强调了香豆素,特别是化合物 和 作为有效抗菌剂的潜力,并为生物活性分子的设计提供了关键见解。

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