| Literature DB >> 21316237 |
Baker Jawabrah Al-Hourani1, Sai Kiran Sharma, Jonathan Y Mane, Jack Tuszynski, Vickie Baracos, Torsten Kniess, Mavanur Suresh, Jens Pietzsch, Frank Wuest.
Abstract
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 IC(50) values ranging from 0.42 to 8.1 mM for COX-1 and 2.0 to 200 μM for COX-2. Most potent compound 3c (IC(50) (COX-2)=2.0 μM) was further used in molecular modeling docking studies.Entities:
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Year: 2011 PMID： 21316237 DOI： 10.1016/j.bmcl.2011.01.057
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823