Article
Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 7. 8-Arylethyldipyridodiazepinones as potent broad-spectrum inhibitors of wild-type and mutant enzymes.
Journal of medicinal chemistry - 30 Jul 1998
Klunder J M, Hoermann M, Cywin C L, David E, Brickwood J R, Schwartz R, Barringer K J, Pauletti D, Shih C K, Erickson D A, Sorge C L, Joseph D P, Hattox S E, Adams J, Grob P M
Abstract excerpt
Like other nonnucleoside inhibitors of HIV-1 reverse transcriptase, the dipyridodiazepinone nevirapine (Viramune, 1) selects for drug resistant variants of HIV-1, both in cell culture and in patients. In particular, the mutation of residue 181 from tyrosine to cysteine (Y181C) is associated with...
Topics
- Amino Acid Substitution
- Antiviral Agents
- Azepines
- Cell Line, Transformed
- Drug Resistance, Microbial
- HIV Reverse Transcriptase
- HIV-1
- Humans
- In Vitro Techniques
- Microsomes, Liver
- Mutation
- Nevirapine
- Pyridines