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Synthesis and studies of new 2-(coumarin-4-yloxy)-4,6-(substituted)-S-triazine derivatives as potential anti-HIV agents.

Archiv der Pharmazie (2009-05-06)
Dharmesh H Mahajan, Christophe Pannecouque, Erik De Clercq, Kishor H Chikhalia
RÉSUMÉ

Novel 2-(coumarin-4-yloxy)-4,6-(substituted)-s-triazine derivatives i. e., diaryltriazine (DATA) are reported as novel non-nucleoside reverse transcriptase inhibitors (NNRTIs), were synthesized and their activities against human immunodeficiency virus HIV-1 (III-B), HIV-2 (ROD), and the double RT mutant HIV-1 (K103N and Y181C) were assessed. Modifications at positions 4 and 6 of the coumarinyl-triazine scaffold generated interesting derivatives displaying good to moderate anti-HIV activity against selected HIV strains as compared to nevirapine and efavirenz. The synthesized compounds were characterized by FTIR, (1)H-NMR, and mass spectral data together with elemental analysis.

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4-Hydroxycoumarin, 98%