Article
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
Journal of medicinal chemistry - 10 Dec 2009
Guillemont Jérôme, Benjahad Abdellah, Oumouch Said, Decrane Laurence, Palandjian Patrice, Vernier Daniel, Queguiner Laurence, Andries Koen, de Béthune Marie-Pierre, Hertogs Kurt, Grierson David S, Nguyen Chi Hung
Abstract excerpt
A series of C-5 methyl substituted 4-arylthio- and 4-aryloxy-3-iodopyridin-2(1H)-ones has been synthesized as new pyridinone analogues for their evaluation as anti-HIV inhibitors. The optimization at the 5-position was developed through an efficient use of the key intermediates 5-ethoxycarbonyl- and 5-cyano-pyridin-2(1H)-ones (14 and 15). Biological studies revealed that several compounds show potent HIV-1...
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