Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 6, Pages 1823-1826Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.01.057
Keywords
Cyclooxygenase; COX-2 inhibitors; 1,5-Diaryl-tetrazoles
Categories
Funding
- Dianne and Irving Kipnes Foundation
- Canadian Institute for Health Research (CIHR)
Ask authors/readers for more resources
A series of 1,5-diaryl-substituted tetrazole derivatives was synthesized via conversion of readily available diaryl amides into corresponding imidoylchlorides followed by reaction with sodium azide. All compounds were evaluated by cyclooxygenase (COX) assays in vitro to determine COX-1 and COX-2 inhibitory potency and selectivity. Tetrazoles 3a-e showed IC50 values ranging from 0.42 to 8.1 mM for COX-1 and 2.0 to 200 mu M for COX-2. Most potent compound 3c (IC50 (COX-2) = 2.0 mu M) was further used in molecular modeling docking studies. (C) 2011 Elsevier Ltd. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available