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Discovery and crystallography of bicyclic arylaminoazines as potent inhibitors of HIV-1 reverse transcriptase.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2015 Nov 01; Vol. 25 (21), pp. 4824-4827. Date of Electronic Publication: 2015 Jul 09. - Publication Year :
- 2015
-
Abstract
- Non-nucleoside inhibitors of HIV-1 reverse transcriptase (HIV-RT) are reported that incorporate a 7-indolizinylamino or 2-naphthylamino substituent on a pyrimidine or 1,3,5-triazine core. The most potent compounds show below 10 nanomolar activity towards wild-type HIV-1 and variants bearing Tyr181Cys and Lys103Asn/Tyr181Cys resistance mutations. The compounds also feature good aqueous solubility. Crystal structures for two complexes enhance the analysis of the structure-activity data.<br /> (Copyright © 2015 Elsevier Ltd. All rights reserved.)
- Subjects :
- Anti-HIV Agents chemical synthesis
Azabicyclo Compounds chemical synthesis
Azabicyclo Compounds chemistry
Bridged Bicyclo Compounds chemical synthesis
Bridged Bicyclo Compounds chemistry
Cell Line
Cell Proliferation drug effects
Dose-Response Relationship, Drug
HIV Reverse Transcriptase metabolism
Humans
Models, Molecular
Molecular Structure
Reverse Transcriptase Inhibitors chemical synthesis
Solubility
Structure-Activity Relationship
Triazines chemical synthesis
Triazines chemistry
Anti-HIV Agents chemistry
Anti-HIV Agents pharmacology
Azabicyclo Compounds pharmacology
Bridged Bicyclo Compounds pharmacology
Drug Discovery
HIV drug effects
HIV Reverse Transcriptase antagonists & inhibitors
Reverse Transcriptase Inhibitors chemistry
Reverse Transcriptase Inhibitors pharmacology
Triazines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 25
- Issue :
- 21
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 26166629
- Full Text :
- https://doi.org/10.1016/j.bmcl.2015.06.074