Non-nucleoside reverse transcriptase inhibitors (Part 18): synthesis and anti-HIV activity of 4-allylamino or 4-azido substituted diaryltriazines.
- Author:
Yuan-Zhen XIONG
1
;
Hai-Rong HU
;
Fen-Er CHEN
;
Jan BALZARINI
;
Christophe PANNECOUQUE
;
Erik de CLERCQ
Author Information
1. School of Pharmacy, Fudan University, Shanghai, China.
- Publication Type:Journal Article
- MeSH:
Anti-HIV Agents;
chemical synthesis;
chemistry;
pharmacology;
Catalytic Domain;
HIV-1;
drug effects;
Inhibitory Concentration 50;
Molecular Structure;
Reverse Transcriptase Inhibitors;
chemical synthesis;
chemistry;
pharmacology;
Triazines;
chemical synthesis;
chemistry;
pharmacology
- From:
Acta Pharmaceutica Sinica
2009;44(2):145-149
- CountryChina
- Language:English
-
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 micromol x L(-1), SI = 6,475) and the double mutant strain (IC50 = 9.39 micromol x L(-1)) in the micromolar range, which was more potent than nevirapine.
