A series of C-5 methyl substituted 4-arylthio-and 4-aryloxy-3-iodopyridin-2 (1 H)-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 (1 H)-ones (14 and 15). Biological studies revealed that several compounds show potent HIV-1 reverse transcriptase ...
