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Synthesis and Biological Evaluations of Sulfanyltriazoles as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors
- Source :
- ChemInform. 37
- Publication Year :
- 2006
- Publisher :
- Wiley, 2006.
-
Abstract
- A novel sulfanyltriazole was discovered as an HIV-1 non-nucleoside reverse transcriptase inhibitor via HTS using a cell-based assay. Chemical modifications and molecular modeling studies were carried out to establish its SAR and understand its interactions with the enzyme. These modifications led to the identification of sulfanyltriazoles with low nanomolar potency for inhibiting HIV-1 replication and promising activities against selected NNRTI resistant mutants. These novel and potent sulfanyltriazoles could serve as advanced leads for further optimization.
- Subjects :
- Models, Molecular
Molecular model
Anti-HIV Agents
Chemistry, Pharmaceutical
Clinical Biochemistry
Cell
Human immunodeficiency virus (HIV)
Pharmaceutical Science
Virus Replication
medicine.disease_cause
Biochemistry
Chemical synthesis
Nucleoside Reverse Transcriptase Inhibitor
Inhibitory Concentration 50
Drug Discovery
Drug Resistance, Viral
medicine
Potency
Enzyme Inhibitors
Molecular Biology
chemistry.chemical_classification
biology
Sulfur Compounds
Reverse-transcriptase inhibitor
Organic Chemistry
Temperature
General Medicine
Triazoles
Nucleotidyltransferase
biology.organism_classification
In vitro
medicine.anatomical_structure
Enzyme
Models, Chemical
chemistry
Enzyme inhibitor
Drug Design
Lentivirus
Mutation
biology.protein
HIV-1
Molecular Medicine
Reverse Transcriptase Inhibitors
Resistant mutants
medicine.drug
Subjects
Details
- ISSN :
- 15222667 and 09317597
- Volume :
- 37
- Database :
- OpenAIRE
- Journal :
- ChemInform
- Accession number :
- edsair.doi.dedup.....6576c002f72280e2fe6724d063fd37e8