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Information Journal Paper

Title

MICROWAVE ASSISTED SYNTHESIS, PHARMACOLOGICAL ACTIVITIES, AND MOLECULAR DOCKING STUDIES OF ETHYL 2-[2-SUBSTITUTED-4-(THIOPHENYL) THIAZOLYL] ACETATES

Pages

  1379-1395

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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    APA: Copy

    VEERABHADRA ATTIMARAD, MAHESH, ABDOU KHEDR, MOHAMMED, & ALDHUBIAB, BANDAR ESSA. (2017). MICROWAVE ASSISTED SYNTHESIS, PHARMACOLOGICAL ACTIVITIES, AND MOLECULAR DOCKING STUDIES OF ETHYL 2-[2-SUBSTITUTED-4-(THIOPHENYL) THIAZOLYL] ACETATES. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), 16(4), 1379-1395. SID. https://sid.ir/paper/288733/en

    Vancouver: Copy

    VEERABHADRA ATTIMARAD MAHESH, ABDOU KHEDR MOHAMMED, ALDHUBIAB BANDAR ESSA. MICROWAVE ASSISTED SYNTHESIS, PHARMACOLOGICAL ACTIVITIES, AND MOLECULAR DOCKING STUDIES OF ETHYL 2-[2-SUBSTITUTED-4-(THIOPHENYL) THIAZOLYL] ACETATES. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR)[Internet]. 2017;16(4):1379-1395. Available from: https://sid.ir/paper/288733/en

    IEEE: Copy

    MAHESH VEERABHADRA ATTIMARAD, MOHAMMED ABDOU KHEDR, and BANDAR ESSA ALDHUBIAB, “MICROWAVE ASSISTED SYNTHESIS, PHARMACOLOGICAL ACTIVITIES, AND MOLECULAR DOCKING STUDIES OF ETHYL 2-[2-SUBSTITUTED-4-(THIOPHENYL) THIAZOLYL] ACETATES,” IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), vol. 16, no. 4, pp. 1379–1395, 2017, [Online]. Available: https://sid.ir/paper/288733/en

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