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Non-nucleoside reverse transcriptase inhibitors (Part 18): synthesis and anti-HIV activity of 4-allylamino or 4-azido substituted diaryltriazines / 药学学报
Acta Pharmaceutica Sinica ; (12): 145-149, 2009.
Article in English | WPRIM | ID: wpr-232582
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.
Subject(s)
Full text: Available Index: WPRIM (Western Pacific) Main subject: Pharmacology / Triazines / Molecular Structure / Chemistry / HIV-1 / Reverse Transcriptase Inhibitors / Anti-HIV Agents / Inhibitory Concentration 50 / Catalytic Domain Language: English Journal: Acta Pharmaceutica Sinica Year: 2009 Type: Article

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Full text: Available Index: WPRIM (Western Pacific) Main subject: Pharmacology / Triazines / Molecular Structure / Chemistry / HIV-1 / Reverse Transcriptase Inhibitors / Anti-HIV Agents / Inhibitory Concentration 50 / Catalytic Domain Language: English Journal: Acta Pharmaceutica Sinica Year: 2009 Type: Article