Seth, Kapileswar ; Garg, Sanjeev K. ; Kumar, Raj ; Purohit, Priyank ; Meena, Vachan S. ; Goyal, Rohit ; Banerjee, Uttam C. ; Chakraborti, Asit K. (2014) 2-(2-arylphenyl)benzoxazole as a novel anti-inflammatory scaffold: synthesis and biological evaluation ACS Medicinal Chemistry Letters, 5 (5). pp. 512-516. ISSN 1948-5875
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Official URL: http://pubs.acs.org/doi/abs/10.1021/ml400500e
Related URL: http://dx.doi.org/10.1021/ml400500e
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.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to American Chemical Society. |
| Keywords: | 2-(2-Arylphenyl)Benzoxazoles; 3D QSAR; Cyclooxygenase-2 Selective; In Vivo Potency; Novel Anti-Inflammatory Scaffold |
| ID Code: | 100253 |
| Deposited On: | 20 Jan 2017 09:31 |
| Last Modified: | 20 Jan 2017 09:31 |
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