具有抗HIV-1逆转录酶活性的新型2-氯-8-芳基硫甲基二吡啶并二氮杂卓酮衍生物
Novel 2-chloro-8-arylthiomethyldipyridodiazepinone derivatives with activity against HIV-1 reverse transcriptase.
作者信息
Khunnawutmanotham Nisachon, Chimnoi Nitirat, Saparpakorn Patchareenart, Pungpo Pornpan, Louisirirotchanakul Suda, Hannongbua Supa, Techasakul Supanna
机构信息
Chulabhorn Research Institute, Vibhavadee-Rangsit Highway, Bangkok 10210, Thailand.
出版信息
Molecules. 2007 Feb 20;12(2):218-30. doi: 10.3390/12020218.
Abstract
Based on the molecular modeling analysis against Y181C HIV-1 RT, dipyridodiazepinone derivatives containing an unsubstituted lactam nitrogen and 2-chloro-8-arylthiomethyl were synthesized via an efficient route. Some of them were evaluated for their antiviral activity against HIV-1 RT subtype E and were found to exhibit virustatic activity comparable to some clinically used therapeutic agents.
摘要
基于针对Y181C HIV-1逆转录酶的分子模拟分析，通过一条高效路线合成了含有未取代内酰胺氮和2-氯-8-芳基硫甲基的二吡啶并二氮杂卓酮衍生物。对其中一些衍生物进行了针对HIV-1 RT E亚型的抗病毒活性评估，发现它们表现出与一些临床使用的治疗药物相当的病毒抑制活性。
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