Iranian Journal of Pharmaceutical Research | |
Microwave Assisted Synthesis, Pharmacological Activities, and Molecular Docking Studies of Ethyl 2-[2-substituted-4-(thiophenyl)thiazolyl] acetates | |
关键词: Analgesic; Anti-inflammatory; Antioxidant; molecular modeling; Synthesis; Thiazole acetates; | |
DOI : | |
学科分类:社会科学、人文和艺术(综合) | |
来源: Shaheed Beheshti Medical University * School of Pharmacy | |
【 摘 要 】
A series of ethyl 2-[2-arylamino-4-(thiophen-2-yl)thiazol-5-yl] acetates (5a-5k) and ethyl 2-[2-(arylhydrazino)-4-(thiophen-2-yl)thiazol-5-yl] acetates (9a-9g) were synthesized and screened for their anti-inflammatory, analgesic, and antioxidant activities. In vivo test results showed that the compounds with halogen substitution (5c, 5g, 5h, 5i and 5j) at the para position on the 2-aryl amino group exhibited good anti-inflammatory and analgesic activities, similar to that of indomethacin and aspirin, respectively. The ethyl 2-[2-(arylhydrazino)-4-(thiophen-2-yl)thiazol-5-yl] acetates (9a-9g) showed better anti-oxidant activity than compounds 5a-5k, comparable to ascorbic acid. However, these compounds showed moderate to weak anti-inflammatory and analgesic activities. Further, a molecular docking study was performed to predict the possible binding modes on cyclooxygenase-1 (COX-1) and COX-2 for the tested compounds. Good correlation was observed between the anti-inflammatory activity of the compounds and the results of the binding modes in COX-2
【 授权许可】
CC BY
【 预 览 】
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RO201904282616587ZK.pdf | 1009KB | download |