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

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

  • Bioorg Med Chem Lett. 2007 Feb 1;17(3):712-6. doi: 10.1016/j.bmcl.2006.10.082.
Abdellah Benjahad 1,  Said Oumouch,  Jerôme Guillemont,  Elisabeth Pasquier,  Dominique Mabire,  Koen Andries,  Chi Hung Nguyen,  David S Grierson
Affiliations

Affiliation

  • 1 UMR 176 CNRS-Institut Curie, Laboratoire de Pharmacochimie, Section de Recherche, Batiment 110, Centre Universitaire, 91405 Orsay, France. Abdellah.Benjahad@curie.u-psud.fr
PMID: 17157017 DOI: 10.1016/j.bmcl.2006.10.082
Abstract

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.

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