Author(s):
Ahmed H. Abdelazeem, Asmaa G. Safi El-Din, Mohammed T. El-Saadi, Samir M. El-Moghazy, Noha H. Amin
Email(s):
samirelmoghazy@gmail.com , ahmed.abdelazeem@pharm.bsu.edu.eg
DOI:
10.5958/0974-360X.2020.00751.9 
Address:
Ahmed H. Abdelazeem1,2*, Asmaa G. Safi El-Din1, Mohammed T. El-Saadi1, Samir M. El-Moghazy3*, Noha H. Amin1
1Department of Medicinal Chemistry, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62514, Egypt.
2Clinical Pharmacy Program, College of Health Sciences, Al-Rayan Colleges, Medinah 42541, Saudi Arabia.
3Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.
*Corresponding Author
Published In:
Volume - 13,
Issue - 9,
Year - 2020
ABSTRACT:
A novel series of diarylpyrazole/triazole derivatives linked to 1,3,4-oxadiazole moiety was synthesized and evaluated in vitro against COX-1/COX-2 enzymes and in vivo for their both anti-inflammatory/analgesic activities utilizing carrageenan-induced paw edema technique and Acetic-acid induced writhing procedure, respectively. The results revealed that compound 13a with adamantyl residue linked to 1,5-diaryl pyrazole showed the highest anti-inflammatory activity comparing with the other derivatives in the series. In comparison to celecoxib, 13a exhibited approximately half the anti-inflammatory activity and selectivity against COX-2 isoenzyme (EI% = 39.18 and IC50 (COX-2) = 2.52 µM for 13a; EI% = 82.71 and IC50 (COX-2) = 0.95 µM for celecoxib). Finally, the binding interactions of 13a into the active site of COX-2 isozyme was explained by performing a docking study.
Cite this article:
Ahmed H. Abdelazeem, Asmaa G. Safi El-Din, Mohammed T. El-Saadi, Samir M. El-Moghazy, Noha H. Amin. Design, Synthesis and Biological Evaluation of Diarylpyrazole/Triazole Bearing 1,3,4- Oxadiazole Moiety as COXs inhibitors Endowed with Potential Anti-Inflammatory and Analgesic Activities. Research J. Pharm. and Tech 2020; 13(9):4255-4262. doi: 10.5958/0974-360X.2020.00751.9
Cite(Electronic):
Ahmed H. Abdelazeem, Asmaa G. Safi El-Din, Mohammed T. El-Saadi, Samir M. El-Moghazy, Noha H. Amin. Design, Synthesis and Biological Evaluation of Diarylpyrazole/Triazole Bearing 1,3,4- Oxadiazole Moiety as COXs inhibitors Endowed with Potential Anti-Inflammatory and Analgesic Activities. Research J. Pharm. and Tech 2020; 13(9):4255-4262. doi: 10.5958/0974-360X.2020.00751.9 Available on: https://www.rjptonline.org/AbstractView.aspx?PID=2020-13-9-39
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