Design,synthesis and biological evaluation of benzimidazole/benzothiazole and benzoxazole derivatives as cyclooxygenase inhibitors |
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Authors: | Paramashivappa R Phani Kumar P Subba Rao P V Srinivasa Rao A |
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Institution: | Vittal Mallya Scientific Research Foundation, PO Box #406, K. R. Road, Bangalore 560 004, India. |
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Abstract: | We have synthesised a series of 2-2-alkoxy-6-pentadecylphenyl)methyl]thio]-1H-benzimidazoles/benzothiazoles and benzoxazoles from anacardic acid and investigated their ability to inhibit human cyclooxygenase-2 enzyme (COX-2). The active compounds were screened for cyclooxygenase-1 (COX-1) inhibition. Compound 13 is 384-fold and 19 is more than 470-fold selective towards COX-2 compared to COX-1. Thus, this class of compounds may serve as excellent candidates for selective COX-2 inhibition. |
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