Home Articles List Article Information
Iranian Journal of Pharmaceutical Research
Journal Archive
Volume Volume 16 (2017)
Volume Volume 15 (2016)
Volume Volume 14 (2015)
Volume Volume 13 (2014)
Volume Volume 12 (2013)
Volume Volume 11 (2012)
Volume Volume 10 (2011)
Volume Volume 9 (2010)
Volume Volume 8 (2009)
Volume Volume 7 (2008)
Volume Volume 6 (2007)
Volume Volume 5 (2006)
Volume Volume 4 (2005)
Volume Volume 3 (2004)
Volume Volume 2 (2003)
Volume Volume 1 (2002)
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(autumn 2017). Iranian Journal of Pharmaceutical Research, (), -.
Mahesh V Attimarad; Mohammed A Khedr; Bander E Aldhubiab. "Microwave Assisted Synthesis, Pharmacological Activities, and Molecular Docking Studies of Ethyl 2-[2-substituted-4-(thiophenyl)thiazolyl] acetates(autumn 2017)". Iranian Journal of Pharmaceutical Research, , , 2017, -.
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(autumn 2017)', Iranian Journal of Pharmaceutical Research, (), pp. -.
Attimarad, M., Khedr, M., Aldhubiab, B. Microwave Assisted Synthesis, Pharmacological Activities, and Molecular Docking Studies of Ethyl 2-[2-substituted-4-(thiophenyl)thiazolyl] acetates(autumn 2017). Iranian Journal of Pharmaceutical Research, 2017; (): -.

Microwave Assisted Synthesis, Pharmacological Activities, and Molecular Docking Studies of Ethyl 2-[2-substituted-4-(thiophenyl)thiazolyl] acetates(autumn 2017)

Articles in Press, Accepted Manuscript , Available Online from 02 September 2017  XML PDF (689 K)
Document Type: Research article
Authors
Mahesh V Attimarad 1; Mohammed A Khedr2; Bander E Aldhubiab3
1College of Clinical Pharmacy, King Faisal University, P.O 400
2College of Clinical Pharmacy, King Faisal University.
3College of Clinical Pharmacy, King Faisal University
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
Keywords
Analgesic; Anti-inflammatory; Antioxidant; molecular modeling; Synthesis; Thiazole acetates
Main Subjects
Medicinal chemistry
Statistics
Article View: 135
PDF Download: 297