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Synthesis and biological evaluation of triazolothienopyrimidine derivatives as novel HIV-1 replication inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Jan 01; Vol. 23 (1), pp. 153-7. Date of Electronic Publication: 2012 Nov 12. - Publication Year :
- 2013
-
Abstract
- We identified a novel class of triazolothienopyrimidine (TTPM) compounds as potent HIV-1 replication inhibitors during a high-throughput screening campaign that evaluated more than 200,000 compounds using a cell-based full replication assay. Herein, we report the optimization of the antiviral activity in a cell-based assay system leading to the discovery of aryl-substituted TTPM derivatives (38, 44, and 45), which exhibited significant inhibition of HIV-1 replication with acceptable safety margins. These novel and potent TTPMs could serve as leads for further development.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)
- Subjects :
- Anti-HIV Agents chemistry
Anti-HIV Agents pharmacology
Cell Line
Drug Evaluation, Preclinical
HIV-1 drug effects
High-Throughput Screening Assays
Humans
Pyrimidines chemical synthesis
Pyrimidines pharmacology
Structure-Activity Relationship
Virus Replication drug effects
Anti-HIV Agents chemical synthesis
HIV-1 metabolism
Pyrimidines chemistry
Triazoles chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 23
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 23206860
- Full Text :
- https://doi.org/10.1016/j.bmcl.2012.10.134