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Synthesis, biological evaluation and molecular modeling studies of quinolonyl diketo acid derivatives: new structural insight into the HIV-1 integrase inhibition.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2011 May; Vol. 46 (5), pp. 1749-56. Date of Electronic Publication: 2011 Feb 22. - Publication Year :
- 2011
-
Abstract
- New quinolonyl diketo acid compounds bearing various substituents at position 6 of the quinolone scaffold were designed and synthesized as potential HIV-1 integrase inhibitors. These new compounds were evaluated for their antiviral and anti-integrase activity and showed inhibitory potency similar to that of 6-bromide analog 2. Molecular modeling and docking studies were performed to rationalize these data and to provide a detailed understanding of the mechanism of inhibition for this class of compounds.<br /> (Copyright © 2011 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Anti-HIV Agents chemical synthesis
Anti-HIV Agents chemistry
Catalytic Domain drug effects
Dose-Response Relationship, Drug
Drug Design
HIV Integrase chemistry
HIV Integrase Inhibitors chemical synthesis
HIV Integrase Inhibitors chemistry
Keto Acids chemical synthesis
Keto Acids chemistry
Models, Molecular
Molecular Structure
Quinolones chemical synthesis
Quinolones chemistry
Stereoisomerism
Structure-Activity Relationship
Anti-HIV Agents pharmacology
HIV drug effects
HIV Integrase metabolism
HIV Integrase Inhibitors pharmacology
Keto Acids pharmacology
Quinolones pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 46
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 21385662
- Full Text :
- https://doi.org/10.1016/j.ejmech.2011.02.028