2. Academic Validation
  3. 3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase

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

  • Bioorg Med Chem Lett. 2003 Dec 15;13(24):4309-12. doi: 10.1016/j.bmcl.2003.09.045.
Abdellah Benjahad 1,  Jérôme Guillemont,  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: 14643315 DOI: 10.1016/j.bmcl.2003.09.045
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 IC(50)=1-45 nM against wild type HIV-1 and a panel of six major simple/double HIV mutant strains.

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