XIONG Yuan-Zhen, Hu-Hai-Rong, Chen-Fen-Er, Jan Balzarini, Christophe Pannecouque, Erik De Clercq. Non-nucleoside reverse transcriptase inhibitors (Part 18): Synthesis and anti-HIV activity of 4-allylamino or 4-azido substituted diaryltriazinesJ. 药学学报, 2009,44(2): 145-149.
Citation: XIONG Yuan-Zhen, Hu-Hai-Rong, Chen-Fen-Er, Jan Balzarini, Christophe Pannecouque, Erik De Clercq. Non-nucleoside reverse transcriptase inhibitors (Part 18): Synthesis and anti-HIV activity of 4-allylamino or 4-azido substituted diaryltriazinesJ. 药学学报, 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

  • 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 = 6 475) and the double mutant strain (IC50 = 9.39 μmol×L-1) in the micromolar range, which was more potent than nevirapine.

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