迈向新的COX-1选择性抑制剂更新的构效关系研究

Title:Update on SAR Studies Toward New COX-1 Selective Inhibitors

Volume: 22 Issue: 37

Author(s): Paola Vitale, Antonio Scilimati and Maria Grazia Perrone

Affiliation:

关键词: 环氧合酶-1，环氧合酶-2，构效关系，二芳基杂环化合物，苯甲酰苯胺，芳基丙酸，二苯乙烯，非甾体抗炎药。

摘要: Few selective cyclooxygenase-1 (COX-1) inhibitors have been described up to now, although recent studies underlined the involvement of COX-1 in the carcinogenesis, pathogenesis of neuroinflammation, cardiovascular diseases and pain. Among the known COX-1 inhibitors none proved to be a good drug candidate, with the exception of mofezolac, that is clinically used as an analgesic drug. New selective inhibitors were very often discovered as a minor achievement during SAR investigations to discover selective COX-2 inhibitors (COXIBs). After a recognition of the new COX-1 inhibitors synthesized in the last five years, it was attempted to draw, for each chemical class, a structure which might highlight the determinant molecular features able to switch the selectivity towards the COX-1 isoform. Overall, this review could constitute a tool to a better design of novel selective COX-1 inhibitors, to be used in a disease theranostic approach targeting COX-1.

Cite this article as:

Paola Vitale, Antonio Scilimati and Maria Grazia Perrone , Update on SAR Studies Toward New COX-1 Selective Inhibitors, Current Medicinal Chemistry 2015; 22 (37) . https://dx.doi.org/10.2174/0929867322666151029104717