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    2-(2-Arylphenyl) benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation

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    Date
    2014
    Author
    Seth, Kapileswar
    Garg, Sanjeev K.
    Kumar, Raj
    Purohit, Priyank
    Meena, Vachan S.
    Goyal, Rohit
    Banerjee, Uttam C.
    Chakraborti, Asit K.
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    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.
    Journal
    ACSMedicinal Chemistry Letters
    Access Type
    Open Access
    URI
    http://210.212.34.21/handle/32116/2333
    URL
    https://pubs.acs.org/doi/abs/10.1021/ml400500e
    DOI
    10.1021/ml400500e
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    • Pharmaceutical Sciences and Natural Products-Research Publications [135]

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    Initiatives by University Library 
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