摘要
治疗艾滋病的逆转录酶抑制剂主要包括核苷逆转录酶抑制剂(NRTIs,如齐多夫定)和非核苷逆转录酶抑制剂(NNRTIs,如奈韦拉平)。目前至少有30多类非核苷类化合物被发现具有选择性抑制HIV-1逆转录酶的作用,其中已经获得美国FDA批准上市的包括奈韦拉平、地拉夫定和埃法韦伦,还有一些品种正在进行临床试验,其中效果较好的包括MKC-442、trovirdine、loviride等。“第一代”NNRTIs的缺点是容易使病毒产生变异,出现耐药性。“第二代”NNRTIs则活性谱广,不容易产生耐药的变异病毒。属于“第二代”NNRTIs的化合物除了埃法韦伦外,还包括埃法韦伦的衍生物DPC083,咪唑衍生物capravirine,二芳基嘧啶类化合物etravirine、rilpivirine。此外,还有一些喹喔啉、吡嗪酮类、烯基二芳基甲烷等也表现出很好的抗HIV活性。相信在不久的将来,将有更多更有效的非核苷逆转录酶抑制剂为人类的健康带来福音。
Upon the chemotherapy of HIV, the use of reverse transcriptase （RT） inhibitors is essential. RT inhibitors are divided into two main classes： nucleoside reverse transcriptase inhibitors （NRTIs）, such as zidovudine （AZT）, and non-nucleoside reverse transcriptase inhibitors （NNRTIs） , such as nevirapine （Viramune）. More than 30 different classes of NNRTIs have been developed, among them nevirapine, delavirdine and efavirenz are commercialized as anti-HIV drugs. Some compounds, which are currently in clinical trials, show potent anti-HIV activities. Such compounds include MKC-442, trovirdine, loviride. The ＂first generation＂ NNRTIs are suffering from drug resistance, whereas the ＂ second generation＂ NNRTIs shows an improved activity spectrum against the most common NNRTI-resistant HIV variants. Compounds belonging to the ＂second generation＂ NNRTIs include DPC083, capravirine, etravirine, rilpivirine etc. Rilpivirine is up to now the most effective compound against HIV.
出处
《精细化工中间体》
CAS
2006年第3期1-6,共6页
Fine Chemical Intermediates
