2-(2-Arylphenyl) benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation
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Date
2014
Journal Title
Journal ISSN
Volume Title
Publisher
ACS publications
Abstract
The 2-(2-arylphenyl)benzoxazole moiety has been found to be a new and selective ligand for the enzyme cyclooxygenase-2 (COX-2). The 2-(2-arylphenyl)benzoxazoles 3a−m have been synthesized by Suzuki reaction of 2-(2-bromophenyl)benzoxazole. Further synthetic manipulation of 3f and 3i led to 3o and 3n, respectively. The compounds 3g, 3n, and 3o selectively inhibited COX-2 with selectivity index of 3n much better than that of the COX-2 selective NSAID celecoxib. The in vivo anti-inflammatory potency of 3g and 3n is comparable to that of celecoxib and the nonselective NSAID diclofenac at two different doses, and 3o showed better potency compared to these clinically used NSAIDs.
Description
Keywords
2-(2-Arylphenyl)benzoxazoles; 3D QSAR; cyclooxygenase-2 selective; in vivo potency; novel anti-inflammatory scaffold
Citation
Seth, Kapileswar., Garg, Sanjeev K. and Kumar, Raj et. al. (2014) 2-(2-Arylphenyl) benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation. ACSMedicinal Chemistry Letters. Vol. 5, PP. 512�516