Novel nevirapine-like inhibitors with improved activity against NNRTI-resistant HIV: 8-heteroarylthiomethyldipyridodiazepinone derivatives |
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| Authors: | 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 |
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| Affiliation: | Department of Chemistry, Boehringer Ingelheim (Canada) Ltd, Research & Development, 2100 Cunard Street, Laval, Québec, Canada H7S 2G5. cyoakim@lav.boehringer-ingelheim.com |
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| Abstract: | 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. |
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