Acta Pharmaceutica Sinica 2009;44(2):145-149

Non-nucleoside reverse transcriptase inhibitors (Part 18): synthesis and anti-HIV activity of 4-allylamino or 4-azido substituted diaryltriazines.

Yuan-Zhen XIONG 1 ; Hai-Rong HU ; Fen-Er CHEN ; Jan BALZARINI ; Christophe PANNECOUQUE ; Erik de CLERCQ

Affiliations

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Country

China

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.