Modulators of the human CCR5 receptor. Part 1: Discovery and initial SAR of 1-(3,3-diphenylpropyl)-piperidinyl amides and ureas.
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.
Burrows
Jeremy N
JN
Respiratory and Inflammation Research Area, AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire, SK10 4TG, UK.
Cumming
John G
JG
Fillery
Shaun M
SM
Hamlin
Gordon A
GA
Hudson
Julian A
JA
Jackson
Ruth J
RJ
McLaughlin
Sharon
S
Shaw
John S
JS
D000577:Amides / Q000737:chemistry*; D006801:Humans; D010880:Piperidines / Q000737:chemistry / Q000494:pharmacology*; D019713:Receptors, CCR5 / Q000187:drug effects*; D013329:Structure-Activity Relationship; D014508:Urea / Q000737:chemistry*
D000577:Amides; D010880:Piperidines; D019713:Receptors, CCR5; D014508:Urea