喹啉酮酸类HIV-1整合酶抑制剂的研究进展  

Research Progress of Quinolone Acid Derivatives as HIV-1 Integrase Inhibitors

作　　者：罗再刚[1] 徐雪梅[1] 胡利明[2] 

机构地区：[1]安徽理工大学化学工程学院,安徽淮南232001 [2]北京工业大学生命科学与生物工程学院,北京100124

出　　处：《药学进展》2013年第3期97-104,共8页Progress in Pharmaceutical Sciences

基　　金：国家自然科学基金青年科学基金(No.21102003);安徽理工大学人才引进启动基金;安徽理工大学青年教师科学研究基金

摘　　要：整合酶是人类免疫缺陷病毒(HIV)进入宿主细胞复制过程中必不可少的一种酶,而人体组织中无此酶,因此,此酶成为高效、低毒的抗HIV药物研发的理想靶标。简介HIV-1整合酶及其抑制剂的作用机制,分类综述具有二酮酸药效团类似结构的喹啉酮酸类HIV-1整合酶抑制剂的研究进展。Integrase is an essential enzyme for HIV-1 retroviral replication in host cells but it hasn＇t been found in human tissue. Therefore it is a rational target for the development of new anti-HIV drugs with high efficiency and low toxicity. The functional mechanisms of HIV-1 integrase and its inhibitors were briefly introduced. The recent researches on the quinolone acid derivatives with similar pharmacophore of diketo acids as HIV-1 integrase inhibitors were classifiedly reviewed.

关 键 词：HIV-1 整合酶抑制剂 二酮酸 喹啉酮酸类衍生物 构效关系 

分 类 号：R978.7[医药卫生—药品] R914.2[医药卫生—药学]