HIV非核苷类逆转录酶抑制剂研究进展

1引言艾滋病(AIDS)是由人类免疫缺陷病毒(HIV)感染引起的严重疾病。HIV属于RNA逆转录病毒,又分为HIV 1和HIV 2型。这两种类型病毒的基因组在DNA碱基序列方面有着明显的差别,因而相应的逆转录酶和包膜上糖蛋白的结构有所不同。世界上大部分地区的艾滋病人是被病毒HIV 1所感染,现     

新型2-芳硫基-5-碘-6-苄基S-DABOs类化合物的合成及作为非核苷类HIV-1 RT抑制剂的活性评估(英文)

我们设计了一系列新型S-DABOs类目标化合物7a-f,通过简单有效的方法合成了该系列化合物,并进行了逆转录酶活性检测,发现该类化合物具有较好的生物活性,其中化合物7d的IC₅₀值达到了3.64μmol/L,是Nevirapine的IC₅₀值的1/2。     

Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1

GW4511, GW4751, and GW3011 showed IC50 values < or =2 nM against wild type HIV-1 and <10 nM against 16 mutants. They were particularly potent against NNRTI-resistant viruses containing Y181C-, K103N-, and K103N-based double mutations, which account for a significant proportion of the clinical failure of the three currently marketed NNRTIs. The antiviral data together with the favorable pharmacokinetic data of GW4511 suggested that these benzophenones possess attributes of a new NNRTI drug candidate.