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Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity.

Benjahad, Abdellah; Oumouch, Said; Guillemont, Jerôme; Pasquier, Elisabeth; Mabire, Dominique; Andries, Koen; Nguyen, Chi Hung; Grierson, David S.
Bioorg Med Chem Lett; 17(3): 712-6, 2007 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-17157017
As part of a systematic SAR study on the 3-iodo-4-phenoxypyridinone 3 (IOPY) type non-nucleoside reverse transcriptase inhibitors, the analogues 4a-4z bearing different C-3 substituents were synthesized and evaluated for their anti-HIV activity against wild-type HIV-1 and four of the principal HIV mutant strains (K103N, Y181C, Y188L, and I100L). The results show that the 3-vinyl analogue 4j is the only compound which displays anti-HIV activity comparable to IOPY 3, and in this respect represents a possible back-up to this lead molecule.
Selo DaSilva