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Synthesis and evaluation of C2-carbon-linked heterocyclic-5-hydroxy-6-oxo-dihydropyrimidine-4-carboxamides as HIV-1 integrase inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2015 Feb 01; Vol. 25 (3), pp. 717-20. Date of Electronic Publication: 2014 Nov 27. - Publication Year :
- 2015
-
Abstract
- Integration of viral DNA into the host cell genome is an obligatory process for successful replication of HIV-1. Integrase catalyzes the insertion of viral DNA into the target DNA and is a validated target for drug discovery. Herein, we report the synthesis, antiviral activity and pharmacokinetic profiles of several C2-carbon-linked heterocyclic pyrimidinone-4-carboxamides that inhibit the strand transfer step of the integration process.<br /> (Copyright © 2014 Elsevier Ltd. All rights reserved.)
- Subjects :
- Amides chemical synthesis
Amides pharmacokinetics
Animals
HIV Integrase metabolism
HIV Integrase Inhibitors chemistry
HIV Integrase Inhibitors pharmacokinetics
HIV-1 drug effects
Half-Life
Heterocyclic Compounds chemistry
Humans
Male
Pyrimidines chemistry
Rats
Rats, Sprague-Dawley
Structure-Activity Relationship
Amides chemistry
HIV Integrase chemistry
HIV Integrase Inhibitors chemical synthesis
HIV-1 enzymology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 25
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 25529736
- Full Text :
- https://doi.org/10.1016/j.bmcl.2014.11.060