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1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains.
Willoughby, Christopher A; Rosauer, Keith G; Hale, Jeffery J; Budhu, Richard J; Mills, Sander G; Chapman, Kevin T; MacCoss, Malcolm; Malkowitz, Lorraine; Springer, Martin S; Gould, Sandra L; DeMartino, Julie A; Siciliano, Salvatore J; Cascieri, Margaret A; Carella, Anthony; Carver, Gwen; Holmes, Karen; Schleif, William A; Danzeisen, Renee; Hazuda, Daria; Kessler, Joseph; Lineberger, Janet; Miller, Michael; Emini, Emilio A.
Afiliação
  • Willoughby CA; Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. cwilloug@amgen.com
Bioorg Med Chem Lett ; 13(3): 427-31, 2003 Feb 10.
Article em En | MEDLINE | ID: mdl-12565944
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.
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Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piperidinas / Pirrolidinas / Antagonistas dos Receptores CCR5 Limite: Animals / Humans Idioma: En Ano de publicação: 2003 Tipo de documento: Article
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Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piperidinas / Pirrolidinas / Antagonistas dos Receptores CCR5 Limite: Animals / Humans Idioma: En Ano de publicação: 2003 Tipo de documento: Article