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 En
| WPRIM
| ID: wpr-232582
Responsible library:
WPRO
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.
Full text:
1
Index:
WPRIM
Main subject:
Pharmacology
/
Triazines
/
Molecular Structure
/
Chemistry
/
HIV-1
/
Reverse Transcriptase Inhibitors
/
Anti-HIV Agents
/
Inhibitory Concentration 50
/
Catalytic Domain
Language:
En
Journal:
Acta Pharmaceutica Sinica
Year:
2009
Type:
Article