摘要
虽然最近的研究强调的COX-1在癌变神经炎症,心血管疾病和疼痛的介入发病,只有少数选择性环氧合酶-1(COX-1)抑制剂被描述到现在为止。在已知的COX-1抑制剂没有证明是一个好的候选药物,除莫苯佐酸在临床上用作止痛药。通过SAR发现选择性COX-2抑制剂(昔布类),新的选择性抑制剂有了小的成就。识别新的COX-1抑制剂在过去的五年里合成的后,我们试图绘制,对于每个化学类,这可能会能够强调朝COX-1同种型转换的分子特征转变成选择性。总体而言,该综述可构成一个工具,以更好的设计的新的选择性COX-1抑制剂,以便在定位的COX-1的疾病治疗诊断方法中使用
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。
Current Medicinal Chemistry
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.
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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
DOI https://dx.doi.org/10.2174/0929867322666151029104717 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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