3-Iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase

A Benjahad, J Guillemont, K Andries…

Index: Benjahad, Abdellah; Guillemont, Jerome; Andries, Koen; Nguyen, Chi Hung; Grierson, David S. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 24 p. 4309 - 4312

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Citation Number: 33

Abstract

Building upon the potent anti-HIV-1 activities observed for the 3-dimethylamino-4- benzylpyridinone 2, and the corresponding 4-aryloxypyridinone analogue 3, a concise and efficient route to the 3-iodo-4-aryloxypyridinones 14a–c (IOPY's) was developed. This involved reaction of the 4-hydroxy substituted pyridinone 10 with the requisite dichloroiodobenzene reagent 11. IOPY compound 14c is active at IC50= 1–45nM against ...