新一代非核苷类HIV逆转录酶抑制剂TMC125的研究进展  

Progress in the New Generation Nonnucleoside Anti-HIV Reverse Transcriptase Inhibitors-TMC125

作　　者：侯金明[1] 黄山[1] 

机构地区：[1]中国药科大学物理化学教研室,南京210000

出　　处：《有机化学》2006年第12期1733-1738,共6页Chinese Journal of Organic Chemistry

摘　　要：阐述了新一代非核苷类逆转录酶抑制剂(Nonnucleosidereversetranscriptaseinhibitors,NNRTIs)TMC125的发现,抗艾滋病病毒、耐药菌株、I型人类免疫缺陷病毒(Humanimmunodeficiencyvirustype1,HIV-1)M亚型病毒以及和其它药物联合使用的活性,代谢稳定性的研究进展.TMC125除具有一般NNRTIs类药物所具有的优点外还有较高的对抗耐药菌株和HIV-1M亚型病毒活性,与其它药物联合使用成为现在治愈人类免疫缺陷病毒(Humanimmunodeficiencyvi-rus,HIV)新的希望.This article summarizes the development and the activity against human immunodeficiency virus type 1 （HIV-1）, nonnucleoside reverse transcriptase inhibitors （NNRTIs）-resistant viruses and HIV-1 group M subtypes of the new generation NNRTIs-TMC125 as well as its metabolic stability assays and the advantage of its combination with other NNRTIs. Besides the same advantage as other NNRTIs, TMC125 was highly active against mutants. It also showed some activity against a series of HIV-1 group M subtypes. Combining TMC125 with other NNRTIs is a potential route against acquired immunodeficiency syndrome （AIDS）.

关 键 词：TMC125 非核苷类逆转录酶抑制剂 人类免疫缺陷病毒 艾滋病 

分 类 号：TQ464.8[化学工程—制药化工]