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1,3,4-Oxadiazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 2: SAR of the C5 position.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Mar 15; Vol. 19 (6), pp. 1807-10. Date of Electronic Publication: 2009 Jan 30. - Publication Year :
- 2009
-
Abstract
- The use of a 1,3,4-oxadiazole in combination with an 8-hydroxy-1,6-naphthyridine ring system has been shown to deliver potent enzyme and antiviral activity through inhibition of viral DNA integration. This report presents a detailed structure-activity investigation of the C5 position resulting in low nM potency for several analogs with an excellent therapeutic index.
- Subjects :
- Amino Acid Motifs
Anti-HIV Agents pharmacology
Chelating Agents pharmacology
Drug Design
HIV Infections drug therapy
HIV Integrase Inhibitors pharmacology
Humans
Metals chemistry
Models, Chemical
Molecular Structure
Naphthyridines pharmacology
Structure-Activity Relationship
Anti-HIV Agents chemical synthesis
Chemistry, Pharmaceutical methods
HIV Integrase Inhibitors chemical synthesis
Naphthyridines chemical synthesis
Oxadiazoles chemistry
Triazoles chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 19
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 19217284
- Full Text :
- https://doi.org/10.1016/j.bmcl.2009.01.089