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Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2001 Feb 12; Vol. 11 (3), pp. 309-12. - Publication Year :
- 2001
-
Abstract
- 3-Alkoxymethyl- and 3-aryloxymethyl-2-pyridinones were synthesized and evaluated for activity as non-nucleoside reverse transcriptase inhibitors (NNRTIs) of HIV-1. It was found that several compounds were potent inhibitors of HIV-1 with the most potent compound 24 exhibiting an IC90 = 32 nM. Compound 24 also possessed a potent resistance profile as demonstrated by submicromolar IC90s against several clinically meaningful mutant virus strains.
- Subjects :
- Anti-HIV Agents pharmacology
Combinatorial Chemistry Techniques
Cytopathogenic Effect, Viral drug effects
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors pharmacology
Fluorine chemistry
HIV Reverse Transcriptase genetics
HIV-1 drug effects
HIV-1 genetics
Inhibitory Concentration 50
Mutation
Pyridones chemical synthesis
Structure-Activity Relationship
Anti-HIV Agents chemical synthesis
HIV Reverse Transcriptase antagonists & inhibitors
Pyridones pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 11
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 11212098
- Full Text :
- https://doi.org/10.1016/s0960-894x(00)00662-4