1.
Bioorg Med Chem Lett
; 15(22): 5012-5, 2005 Nov 15.
Article
in English
| MEDLINE
| ID: mdl-16154744
ABSTRACT
SAR and DMPK studies led to the identification of substituted N-alkyl-N-[1-(3,3-diphenylpropyl)piperidin-4-yl]-2-phenylacetamides as potent and orally bioavailable ligands for the human CCR5 chemokine receptor.
Subject(s)
Benzeneacetamides/chemistry , Benzeneacetamides/pharmacology , CCR5 Receptor Antagonists , Piperidines/chemistry , Receptors, CCR5/metabolism , Animals , Benzeneacetamides/chemical synthesis , Benzeneacetamides/pharmacokinetics , Biological Availability , Humans , Inhibitory Concentration 50 , Ligands , Molecular Structure , Rats , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 15(1): 25-8, 2005 Jan 03.
Article
in English
| MEDLINE
| ID: mdl-15582404
ABSTRACT
Investigation of weak screening hits led to the identification of N-alkyl-N-[1-(3,3-diphenylpropyl)piperidin-4-yl]-2-phenylacetamides and N-alkyl-N-[1-(3,3-diphenylpropyl)piperidin-4-yl]-N'-benzylureas as potent, selective ligands for the human CCR5 chemokine receptor.