Modulators of the human CCR5 receptor. Part 2: SAR of substituted 1-(3,3-diphenylpropyl)-piperidinyl phenylacetamides.
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.
Cumming
John G
JG
Respiratory & Inflammation Research Area, AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK. john.cumming@astrazeneca.com
Cooper
Anne E
AE
Grime
Ken
K
Logan
Chris J
CJ
McLaughlin
Sharon
S
Oldfield
John
J
Shaw
John S
JS
Tucker
Howard
H
Winter
Jon
J
Whittaker
David
D
D000818:Animals; D044482:Benzeneacetamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D001682:Biological Availability; D065100:CCR5 Receptor Antagonists; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D015394:Molecular Structure; D010880:Piperidines / Q000737:chemistry*; D051381:Rats; D019713:Receptors, CCR5 / Q000378:metabolism*; D013329:Structure-Activity Relationship
D044482:Benzeneacetamides; D065100:CCR5 Receptor Antagonists; D008024:Ligands; D010880:Piperidines; D019713:Receptors, CCR5; C032727:piperidine