4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.

doi:10.1021/jm0408621

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Article

4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.

Journal of medicinal chemistry - 24 Mar 2005

Benjahad Abdellah, Croisy Martine, Monneret Claude, Bisagni Emile, Mabire Dominique, Coupa Sophie, Poncelet Alain, Csoka Imre, Guillemont Jérôme, Meyer Christophe, Andries Koen, Pauwels Rudi, de Béthune Marie-Pierre, Himmel Daniel M, Das Kalyan, Arnold Eddy, Nguyen Chi Hung, Grierson David S

Abstract excerpt

In a program to optimize the anti-HIV activity of the 4-benzyl and 4-benzoyl-3-dimethylaminopyridinones 9 and 10, lead compounds in a new class of highly potent non-nucleoside type inhibitors of HIV-1 reverse transcriptase, modification of the alkyl substitutents at the C-5 and C-6 positions on the pyridinone ring and of the substitutents on the C-3 amino group has been studied. Of the 17 new 5/6-modified...

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PMID: 15771439
DOI: 10.1021/jm0408621

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