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Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 13. Synthesis and profiling of a novel amminium prodrug of the HIV-1 attachment inhibitor BMS-585248.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2013 Feb 28; Vol. 56 (4), pp. 1670-6. Date of Electronic Publication: 2013 Feb 12. - Publication Year :
- 2013
-
Abstract
- In vitro studies suggested that the ammonium salt 2 could be a viable prodrug of the HIV-1 attachment inhibitor 1. Increased systemic exposure of the parent drug 1 following oral administration of the amminium salt 2 when compared to similar studies using solution dosing of the parent compound was observed in the in vivo studies in both rats and dogs. At high doses, the improvement in oral exposure of the parent drug was even more evident, indicating that the increased solubility of the amminium salt 2 can overcome dissolution-limited absorption and demonstrating the potential utility of this compound as a prodrug of 1.
- Subjects :
- Administration, Oral
Animals
Anti-Bacterial Agents pharmacology
Anti-HIV Agents pharmacokinetics
Dogs
Gastrointestinal Tract drug effects
Gastrointestinal Tract metabolism
Gastrointestinal Tract microbiology
HIV-1 physiology
High-Throughput Screening Assays
Humans
Liver metabolism
Male
Piperazines pharmacokinetics
Prodrugs pharmacokinetics
Prodrugs pharmacology
Pyridines pharmacokinetics
Pyrroles pharmacokinetics
Rats
Structure-Activity Relationship
Triazines pharmacokinetics
Triazoles pharmacokinetics
Virus Attachment drug effects
Anti-HIV Agents chemical synthesis
HIV-1 drug effects
Piperazines chemical synthesis
Prodrugs chemical synthesis
Pyridines chemical synthesis
Pyrroles chemical synthesis
Triazines chemical synthesis
Triazoles chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 1520-4804
- Volume :
- 56
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 23374053
- Full Text :
- https://doi.org/10.1021/jm301638a