Back to Search
Start Over
Design and synthesis of novel β-diketo derivatives as HIV-1 integrase inhibitors.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2012 Jan 01; Vol. 20 (1), pp. 177-82. Date of Electronic Publication: 2011 Nov 22. - Publication Year :
- 2012
-
Abstract
- A series of novel β-diketo derivatives which combined the virtues of 1,3-diketo, 1,2,3-triazole and polyhydroxylated aromatics moieties, were designed and synthesized as potential HIV-1 integrase (IN) inhibitors and evaluated their inhibition to the strand transfer process of HIV-1 integrase. The result indicates that 3,4,5-trihydroxylated aromatic derivatives exhibit good inhibition to HIV-1 integrase, but dihydroxylated aromatic derivatives and corresponding methoxy aromatic derivatives appear little inhibition to HIV-1 integrase.<br /> (Copyright © 2011 Elsevier Ltd. All rights reserved.)
- Subjects :
- Enzyme Activation drug effects
HIV Integrase metabolism
HIV Integrase Inhibitors chemistry
HIV-1 drug effects
Humans
Keto Acids chemical synthesis
Keto Acids pharmacology
Structure-Activity Relationship
Triazoles chemistry
Drug Design
HIV Integrase chemistry
HIV Integrase Inhibitors chemical synthesis
HIV Integrase Inhibitors pharmacology
Keto Acids chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 20
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 22154762
- Full Text :
- https://doi.org/10.1016/j.bmc.2011.11.014