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喹诺酮足近年来寻找抗HlV新药的重要结构骨架之一。通过结构修饰,可从中筛选出若干有希望的整合晦抑制剂、逆转录酶抑制剂以及双重(逆转录酶+整合酶)抑制剂。尤其是整合酶抑制制elvitegravir即将上市,引起对抗HIV喹诺酮研发的关注。本文按喹诺酮的结构特征,从2-喹诺酮、4-喹讲酮、β-二酮酸和杂合体着手,综述了近年来这类化合物在抗HIV活性及其构效关系、作用机制等方面的研究进展。
In recent years, quinolone is one of the important structural skeletons for anti-H1V drug. Through structural modification, a number of promising integron inhibitors, reverse transcriptase inhibitors and dual (reverse transcriptase + integrase) inhibitors can be screened out. In particular, the integrase-inhibiting elvitegravir is on the market, raising concerns over the development of HIV quinolones. In this paper, the structural characteristics of quinolones, starting from 2-quinolone, 4-quinolone, β-diketone and hybrids, the recent review of these compounds in anti-HIV activity and its structure-activity relationship, mechanism of action Research progress.