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Bioorg Med Chem Lett ; 16(13): 3533-6, 2006 Jul 01.
Article in English | MEDLINE | ID: mdl-16631366

ABSTRACT

SAR and PK studies led to the identification of N-(1-{(3R)-3-(3,5-difluorophenyl)-3-[4-methanesulfonylphenyl] propyl}piperidin-4-yl)-N-ethyl-2-[4-methanesulfonylphenyl]acetamide as a highly potent and selective ligand for the human CCR5 chemokine receptor with good oral pharmacokinetic properties.


Subject(s)
Acetanilides/chemistry , Acetanilides/pharmacokinetics , CCR5 Receptor Antagonists , Piperidines/chemistry , Piperidines/pharmacology , Sulfones/chemistry , Sulfones/pharmacology , Acetanilides/chemical synthesis , Animals , Crystallography, X-Ray , Dogs , Humans , Models, Molecular , Molecular Structure , Piperidines/chemical synthesis , Rats , Stereoisomerism , Structure-Activity Relationship , Sulfones/chemical synthesis , Time Factors
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