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Scaffold hopping: Exploration of acetanilide-containing uracil analogues as potential NNRTIs
- Source :
- Bioorganic & Medicinal Chemistry. 23:1069-1081
- Publication Year :
- 2015
- Publisher :
- Elsevier BV, 2015.
-
Abstract
- In order to identify novel nonnucleoside inhibitors of HIV-1 reverse transcriptase two series of amide-containing uracil derivatives were designed as hybrids of two scaffolds of previously reported inhibitors. Subsequent biological evaluation confirmed acetamide uracil derivatives 15a–k as selective micromolar NNRTIs with a first generation-like resistance profile. Molecular modeling of the most active compounds 15c and 15i was employed to provide insight on their inhibitory properties and direct future design efforts.
- Subjects :
- Models, Molecular
Molecular model
Anti-HIV Agents
Stereochemistry
Clinical Biochemistry
Drug Evaluation, Preclinical
Pharmaceutical Science
Scaffold hopping
Biochemistry
Cell Line
chemistry.chemical_compound
Amide
Drug Discovery
Humans
Uracil
Molecular Biology
Acetanilide
Biological evaluation
Organic Chemistry
Reverse transcriptase
chemistry
Reverse Transcriptase Inhibitors
Molecular Medicine
Acetanilides
Acetamide
Subjects
Details
- ISSN :
- 09680896
- Volume :
- 23
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....da99410e86219cb5a7b5bc0795f1ca90