二酮酸类HIV-1整合酶抑制剂的研究进展  

Progress on diketo acid HIV-1 integrase inhibitors

作　　者：杨学章[1] 郭长彬[1] 周化[1] 唐朝军[1] 

机构地区：[1]首都师范大学化学系,北京100048

出　　处：《中国药物化学杂志》2009年第5期390-395,共6页Chinese Journal of Medicinal Chemistry

摘　　要：HIV-1整合酶催化前病毒DNA整合进入宿主细胞基因组的过程是病毒复制必不可少的步骤,所以抑制HIV-1整合酶活性是治疗HIV-1感染的合理策略。目前已开发了大量HIV-1整合酶抑制剂,其中一些已进入临床研究阶段,从化学结构看,绝大多数已报道的HIV-1整合酶抑制剂属于二酮酸类或其生物电子等排体。该文对近3年来二酮酸类HIV-1整合酶抑制剂的研究进展做简要综述。HIV-1 integrase catalyzes the integration of proviral DNA into the genome of the host cell,an essential step for viral replication,thus inhibition of integrase catalytic activity represents a rational strategy for the treatment of HIV-1 infection.At present,a lot of HIV-1 integrase inhibitors have been designed and synthesized,and some of them are studied currently in clinical trials.In a view of chemical structure,most of the HIV-1 integrase inhibitors reported belong to the class of diketo acids or their bioisosters.Recent advances on diketo acid HIV-1 integrase inhibitors are reviewed in this paper.

关 键 词：HIV-1整合酶抑制剂 二酮酸类 雷特格韦 艾滋病化学治疗 

分 类 号：R914[医药卫生—药物化学]