Attimarad, M., Khedr, M., Aldhubiab, B. (2017). Microwave Assisted Synthesis, Pharmacological Activities, and Molecular Docking Studies of Ethyl 2-[2-substituted-4-(thiophenyl)thiazolyl] acetates. Iranian Journal of Pharmaceutical Research, 16(4), 1379-1395.
Mahesh Attimarad; Mohammed Khedr; Bander Aldhubiab. "Microwave Assisted Synthesis, Pharmacological Activities, and Molecular Docking Studies of Ethyl 2-[2-substituted-4-(thiophenyl)thiazolyl] acetates". Iranian Journal of Pharmaceutical Research, 16, 4, 2017, 1379-1395.
Attimarad, M., Khedr, M., Aldhubiab, B. (2017). 'Microwave Assisted Synthesis, Pharmacological Activities, and Molecular Docking Studies of Ethyl 2-[2-substituted-4-(thiophenyl)thiazolyl] acetates', Iranian Journal of Pharmaceutical Research, 16(4), pp. 1379-1395.
Attimarad, M., Khedr, M., Aldhubiab, B. Microwave Assisted Synthesis, Pharmacological Activities, and Molecular Docking Studies of Ethyl 2-[2-substituted-4-(thiophenyl)thiazolyl] acetates. Iranian Journal of Pharmaceutical Research, 2017; 16(4): 1379-1395.
Microwave Assisted Synthesis, Pharmacological Activities, and Molecular Docking Studies of Ethyl 2-[2-substituted-4-(thiophenyl)thiazolyl] acetates
College of Clinical Pharmacy, King Faisal University, Al-Ahsa, KSA.
Abstract
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
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