Non-nucleoside reverse transcriptase inhibitors(Part 18): Synthesis and anti-HIV activity of 4-allylamino or 4-azido substituted diaryltriazines
- VernacularTitle:非核苷类逆转录酶抑制剂的研究XVⅢ:4-烯丙基和4-叠氮基取代的三嗪类化合物的合成及抗HIV活性
- Author:
Yuanzhen XIONG
- Publication Type:Journal Article
- Keywords:
non-nucleoside reverse transcriptase inhibitors;
anti-HIV;
4-allyl diaryltriazine;
4-azido diaryl- triazine
- From:
Acta Pharmaceutica Sinica
2009;44(2):145-149
- CountryChina
- Language:Chinese
-
Abstract:
Eight new diaryltriazine derivatives containing 4-allylamino and 4-azido substitutes guided by molecular docking have been designed and synthesized based on our previous work.The evaluation of HIV inhibitory activity demonstrated that all compounds were potent against HIV-1 replication.The most active compound 7c exhibited activity against HIV-1 (IC50=0.034 μmol·L-1,SI=6475)and the double mutant strain (IC50=9.39 μmol·L-1)in the micromolar range, which was more potent than nevirapine.
