Design, synthesis and biological evaluation of benzimidazole/benzothiazole and benzoxazole derivatives as cyclooxygenase inhibitors

R Paramashivappa, PP Kumar, PVS Rao…

文献索引：Paramashivappa; Phani Kumar; Subba Rao; Srinivasa Rao Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 4 p. 657 - 660

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被引用次数: 217

摘要

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 ...