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噻二唑基席夫碱衍生物的合成、生物评价及分子对接研究。

Synthesis, bio-evaluation and molecular docking studies of thiadiazole-based Schiff base derivatives.

机构信息

Department of Chemistry, COMSATS University Islamabad, Islamabad, 45550, Pakistan.

Department of Chemistry, Hazara University, Mansehra, 21120, Pakistan.

出版信息

Future Med Chem. 2024 Feb;16(4):335-348. doi: 10.4155/fmc-2023-0276. Epub 2024 Feb 5.

DOI:10.4155/fmc-2023-0276
PMID:38314616
Abstract

Recently, thiadiazole-containing drugs have gained greater clinical relevance and are being explored for the development of new antidiabetic, antiurease and antimicrobial agents that target drug resistance. The authors disclose the synthesis of -(5-[4-(trifluoromethyl)phenyl]-1,3,4-thiadiazol-2-yl)methanimine derivatives starting from 4-(trifluoromethyl)benzoic acid. All of the synthesized derivatives were evaluated for their biological potential in order to investigate the inhibitory activity against antidiabetic, antiurease and antibacterial profiles. Compounds , and showed excellent inhibitory activities due to the hydrogen bonding presence of -OH, -F and -CF substitutions attached with the phenyl ring. The present study provides potent antidiabetic, antiurease and antimicrobial agents that can be further optimized to discover novel antidiabetic, antiurease drugs.

摘要

最近,含噻二唑的药物在临床相关性方面有了更大的进展,并且正在探索新的抗糖尿病、抗脲酶和抗微生物药物,以针对耐药性。作者披露了从 4-(三氟甲基)苯甲酸开始合成 -(5-[4-(三氟甲基)苯基]-1,3,4-噻二唑-2-基)甲亚胺衍生物的方法。所有合成的衍生物都进行了生物潜力评估,以研究其对糖尿病、抗脲酶和抗菌谱的抑制活性。由于苯环上的 -OH、-F 和 -CF 取代物的氢键存在,化合物 、 和 表现出优异的抑制活性。本研究提供了有效的抗糖尿病、抗脲酶和抗菌剂,可进一步优化以发现新型抗糖尿病、抗脲酶药物。

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