Article
Novel nevirapine-like inhibitors with improved activity against NNRTI-resistant HIV: 8-heteroarylthiomethyldipyridodiazepinone derivatives.
Bioorganic & medicinal chemistry letters - 9 Feb 2004
Yoakim C, Bonneau P R, Déziel R, Doyon L, Duan J, Guse I, Landry S, Malenfant E, Naud J, Ogilvie W W, O'Meara J A, Plante R, Simoneau B, Thavonekham B, Bös M, Cordingley M G
Abstract excerpt
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.
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.
