Novel nevirapine-like inhibitors with improved activity against NNRTI-resistant HIV: 8-heteroarylthiomethyldipyridodiazepinone derivatives
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 profi...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2004-02, Vol.14 (3), p.739-742 |
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| container_title | Bioorganic & medicinal chemistry letters |
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| creator | 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. |
| description | 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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| doi_str_mv | 10.1016/j.bmcl.2003.11.049 |
| format | Article |
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Drug treatments</subject><subject>Pyridines - chemical synthesis</subject><subject>Pyridines - metabolism</subject><subject>Pyridines - pharmacology</subject><subject>Rats</subject><subject>Reverse Transcriptase Inhibitors - chemical synthesis</subject><subject>Reverse Transcriptase Inhibitors - metabolism</subject><subject>Reverse Transcriptase Inhibitors - pharmacology</subject><subject>Structure-Activity Relationship</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2004</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kU9v1DAQxS0EotvCF-CAcoFbgu04joO4oIrSlapFQgVxsxx7QmbJn63tDVo-Ap8ar3al3jjN5ffezLxHyCtGC0aZfLct2tEOBae0LBgrqGiekBUTUuSloNVTsqKNpLlqxI8LchnCllImqBDPyQUTtWBc0RX5u5kXGLIJFvRmhxPkA_6CDKceW4yzD9lvjH2G484n0GXGRlwwHjLz0-AUYrbZfL1f5x4ChmimmN2uv7_PVN5DBD8bfxhij_MIsT8MDncHj252aP5A2jVPkDnwuJjkCeEFedaZIcDL87wi324-3V_f5ndfPq-vP97lljd1zJXkjexKpRpZqYpC2ZrWdZJVDTcGWic4U5QpyTiTUjSVZa6yXNSVhBoaJsor8vbkm1562EOIesRgYRjMBPM-6KTmjPIjyE-g9XMIHjq98zimnzSj-tiA3upjA_rYgGZMpwaS6PXZfd-O4B4l58gT8OYMmGDN0HkzWQyPXCVqRasycR9OHKQsFgSvg0WYLDj0YKN2M_7vjn-kqKch</recordid><startdate>20040209</startdate><enddate>20040209</enddate><creator>Yoakim, C.</creator><creator>Bonneau, P.R.</creator><creator>Déziel, R.</creator><creator>Doyon, L.</creator><creator>Duan, J.</creator><creator>Guse, I.</creator><creator>Landry, S.</creator><creator>Malenfant, E.</creator><creator>Naud, J.</creator><creator>Ogilvie, W.W.</creator><creator>O'Meara, J.A.</creator><creator>Plante, R.</creator><creator>Simoneau, B.</creator><creator>Thavonekham, B.</creator><creator>Bös, M.</creator><creator>Cordingley, M.G.</creator><general>Elsevier Ltd</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20040209</creationdate><title>Novel nevirapine-like inhibitors with improved activity against NNRTI-resistant HIV: 8-heteroarylthiomethyldipyridodiazepinone derivatives</title><author>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.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c297t-86296f388965850e3babdf61592aaebd4218018612166495c1d5c24756e7e9143</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2004</creationdate><topic>Animals</topic><topic>Anti-HIV Agents - chemical synthesis</topic><topic>Anti-HIV Agents - metabolism</topic><topic>Anti-HIV Agents - pharmacology</topic><topic>Antibiotics. 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16 was found to have a good pharmacokinetic profile in spite of poor metabolic stability in rat liver microsomes.
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| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2004-02, Vol.14 (3), p.739-742 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Anti-HIV Agents - chemical synthesis Anti-HIV Agents - metabolism Anti-HIV Agents - pharmacology Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral agents Azepines - chemical synthesis Azepines - metabolism Azepines - pharmacology Biological and medical sciences Drug Resistance, Viral HIV Infections - drug therapy HIV Infections - virology HIV Reverse Transcriptase - chemistry HIV-1 - drug effects HIV-1 - enzymology HIV-1 - genetics Humans Medical sciences Metabolic Clearance Rate Microsomes, Liver - drug effects Microsomes, Liver - metabolism Mutation Nevirapine - chemical synthesis Nevirapine - pharmacology Pharmacology. Drug treatments Pyridines - chemical synthesis Pyridines - metabolism Pyridines - pharmacology Rats Reverse Transcriptase Inhibitors - chemical synthesis Reverse Transcriptase Inhibitors - metabolism Reverse Transcriptase Inhibitors - pharmacology Structure-Activity Relationship |
| title | Novel nevirapine-like inhibitors with improved activity against NNRTI-resistant HIV: 8-heteroarylthiomethyldipyridodiazepinone derivatives |
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