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Naphthyridinone (NTD) integrase inhibitors 4. Investigating N1 acetamide substituent effects with C3 amide groups.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2014 Jul 15; Vol. 24 (14), pp. 3104-7. Date of Electronic Publication: 2014 May 16. - Publication Year :
- 2014
-
Abstract
- A series of N1 acetamide substituted naphthyridinone HIV-1 integrase inhibitors have been explored to understand structure-activity relationships (SAR) with various C3 amide groups. Investigations were evaluated using integrase enzyme inhibition, antiviral activity and protein binding effects to optimize the sub-structures. Lipophilicity was also incorporated to understand ligand lipophilic efficiency as a function of the structural modifications. Three representative analogs were further examined in a peripheral blood mononuclear cell (PBMC) antiviral assay as well as in vitro and in vivo drug metabolism and pharmacokinetic studies.<br /> (Copyright © 2014 Elsevier Ltd. All rights reserved.)
- Subjects :
- Dose-Response Relationship, Drug
HIV Integrase Inhibitors chemical synthesis
HIV Integrase Inhibitors chemistry
Humans
Leukocytes, Mononuclear drug effects
Leukocytes, Mononuclear virology
Molecular Structure
Naphthyridines chemical synthesis
Naphthyridines chemistry
Structure-Activity Relationship
Acetamides chemistry
Amides chemistry
HIV Integrase metabolism
HIV Integrase Inhibitors pharmacology
Naphthyridines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 24
- Issue :
- 14
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 24908608
- Full Text :
- https://doi.org/10.1016/j.bmcl.2014.05.011