HIV-1蛋白酶抑制剂前药的研究进展  

Progress in HIV-1 Protease Inhibitor Prodrugs

作　　者：雷厉军[1] 何煦昌[1] 

机构地区：[1]中国科学院上海生命科学研究院上海药物研究所,上海201203

出　　处：《药学进展》2005年第7期295-301,共7页Progress in Pharmaceutical Sciences

摘　　要：综述HIV1蛋白酶抑制剂前药的研究进展。HIV1蛋白酶抑制剂前药是以HIV1蛋白酶抑制剂为母体,通过引入亲脂性或亲水性基团等结构修饰而得到的一类药物前体,尤其是基于蛋白酶抑制剂和逆转录酶抑制剂为母体药物设计的“双药”型抗HIV1前药,它们能在体内水解释放出母体药物,从而提高母体药物活性及生物利用度,降低其耐药性或交叉耐药性。The progress in HIV-1 protease inhibitor prodrugs was reviewed. The HIV-1 protease inhibitor prodrugs are a kind of precursors derived from structure-modified HIV-1 protease inhibitors by introducing lipophilic or hydrophilic groups, especially including anti-HIV double-drugs—conjugates of HIV-1 protease inhibitors with a reverse transcriptase inhibitor through spontaneously cleavable linkers. These prodrugs can release the parent drug in vivo to improve anti-HIV-1 activity and bioavailability and to reduce the resistance and the cross resistance.

关 键 词：前药 HIV-1蛋白酶抑制剂 逆转录酶抑制剂 抗HIV活性 生物利用度 

分 类 号：R978.7[医药卫生—药品]