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作为环氧合酶抑制剂的苯并咪唑/苯并噻唑和苯并恶唑衍生物的设计、合成及生物学评价

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

作者信息

Paramashivappa R, Phani Kumar P, Subba Rao P V, Srinivasa Rao A

机构信息

Vittal Mallya Scientific Research Foundation, PO Box #406, K. R. Road, Bangalore 560 004, India.

出版信息

Bioorg Med Chem Lett. 2003 Feb 24;13(4):657-60. doi: 10.1016/s0960-894x(02)01006-5.

DOI:10.1016/s0960-894x(02)01006-5
PMID:12639552
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.

摘要

我们从腰果壳液酸合成了一系列2-[[2-烷氧基-6-十五烷基苯基)甲基]硫代]-1H-苯并咪唑/苯并噻唑和苯并恶唑，并研究了它们抑制人环氧化酶-2（COX-2）的能力。对活性化合物进行了环氧化酶-1（COX-1）抑制筛选。与COX-1相比，化合物13对COX-2的选择性为384倍，化合物19对COX-2的选择性超过470倍。因此，这类化合物可能是选择性COX-2抑制的优秀候选物。

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