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1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2003 Feb 10; Vol. 13 (3), pp. 427-31. - Publication Year :
- 2003
-
Abstract
- A new class of 4-(aminoheterocycle)piperidine derived 1,3,4 trisubstituted pyrrolidine CCR5 antagonists is reported. Compound 4a is shown to have good binding affinity (1.8 nM) and antiviral activity in PBMC's (IC(95)=50 nM). Compound 4a also has improved PK properties relative to 1.
- Subjects :
- Animals
Anti-HIV Agents chemical synthesis
CHO Cells
Chemokine CCL4
Cricetinae
Half-Life
HeLa Cells
Humans
Hydrogen Bonding
Macrophage Inflammatory Proteins metabolism
Piperidines pharmacokinetics
Pyrrolidines pharmacokinetics
Rats
CCR5 Receptor Antagonists
Piperidines chemical synthesis
Piperidines pharmacology
Pyrrolidines chemical synthesis
Pyrrolidines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 13
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 12565944
- Full Text :
- https://doi.org/10.1016/s0960-894x(02)00988-5