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1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2003 Jan 06; Vol. 13 (1), pp. 119-23. - Publication Year :
- 2003
-
Abstract
- The 4-(3-phenylprop-1-yl)piperidine moiety of the 1,3,4-trisubstituted pyrrolidine CCR5 antagonist 1 was modified with electron deficient aromatics as well as replacement of the benzylic methylene with sulfones, gem-difluoromethylenes and alcohols in an effort to balance the antiviral potency with reasonable pharmacokinetics.
- Subjects :
- Animals
Anti-HIV Agents pharmacokinetics
Anti-HIV Agents pharmacology
Dogs
Half-Life
Humans
Leukocytes, Mononuclear
Macaca mulatta
Metabolic Clearance Rate
Piperidines chemistry
Pyrrolidines chemical synthesis
Pyrrolidines pharmacology
Radioligand Assay
Rats
Structure-Activity Relationship
Tumor Cells, Cultured
Anti-HIV Agents chemical synthesis
CCR5 Receptor Antagonists
Pyrrolidines pharmacokinetics
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 13
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 12467630
- Full Text :
- https://doi.org/10.1016/s0960-894x(02)00829-6