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Bioorg Med Chem Lett. 2003 Feb 10;13(3):427-31.

1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. cwilloug@amgen.com

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.

PMID:
12565944
DOI:
10.1016/s0960-894x(02)00988-5
[Indexed for MEDLINE]

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