Portal de Periódicos da CAPES

Novel nevirapine-like inhibitors with improved activity against NNRTI-resistant HIV: 8-heteroarylthiomethyldipyridodiazepinone derivatives

2003; Elsevier BV; Volume: 14; Issue: 3 Linguagem: Inglês

10.1016/j.bmcl.2003.11.049

1464-3405

Christiane Yoakim, Pierre Bonneau, Robert Déziel, Louise Doyon, Jianmin Duan, Ingrid Guse, Serge Landry, Éric Malenfant, Julie Naud, William W. Ogilvie, J O'Meara, Raymond Plante, Bruno Simoneau, Bounkham Thavonekham, Michael Bös, Michael G. Cordingley,

Hepatitis C virus research

A series of 8-heteroarylthiomethyldipyridodiazepinone derivatives were prepared and evaluated for their antiviral profile against wild type virus and the important K103N/Y181C mutant as an indicator for broad activity. 2,6-Dimethylpyridine derivative 16 was found to have a good pharmacokinetic profile in spite of poor metabolic stability in rat liver microsomes.