Structure-Based Bioisosterism Yields HIV-1 NNRTIs with Improved Drug-Resistance Profiles and Favorable Pharmacokinetic Properties.
Animals
Anti-HIV Agents
/ metabolism
Cell Line, Tumor
Enzyme Assays
HIV Reverse Transcriptase
/ antagonists & inhibitors
HIV-1
/ drug effects
Humans
Mice
Microbial Sensitivity Tests
Microsomes, Liver
/ metabolism
Molecular Docking Simulation
Mutation
Protein Binding
Pyrimidines
/ metabolism
Reverse Transcriptase Inhibitors
/ metabolism
Thiophenes
/ metabolism
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
14 05 2020
14 05 2020
Historique:
pubmed:
16
4
2020
medline:
3
11
2020
entrez:
16
4
2020
Statut:
ppublish
Résumé
The development of efficacious NNRTIs for AIDS therapy commonly encountered the rapid generation of drug-resistant mutations, which becomes a major impediment to effective anti-HIV treatment. Using a structure-based bioisosterism strategy, a series of piperidine-substituted thiophene[2,3-
Identifiants
pubmed: 32293182
doi: 10.1021/acs.jmedchem.0c00117
doi:
Substances chimiques
Anti-HIV Agents
0
Pyrimidines
0
Reverse Transcriptase Inhibitors
0
Thiophenes
0
reverse transcriptase, Human immunodeficiency virus 1
EC 2.7.7.-
HIV Reverse Transcriptase
EC 2.7.7.49
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM