Design, synthesis, and structure-activity relationship of novel CCR2 antagonists.
A series of novel 1-aminocyclopentyl-3-carboxyamides incorporating substituted tetrahydropyran moieties have been synthesized and subsequently evaluated for their antagonistic activity against the human CCR2 receptor. Among them analog 59 was found to posses potent antagonistic activity.
Kothandaraman
Shankaran
S
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
Donnely
Karla L
KL
Butora
Gabor
G
Jiao
Richard
R
Pasternak
Alexander
A
Morriello
Gregori J
GJ
Goble
Stephen D
SD
Zhou
Changyou
C
Mills
Sander G
SG
Maccoss
Malcolm
M
Vicario
Pasquale P
PP
Ayala
Julia M
JM
Demartino
Julie A
JA
Struthers
Mary
M
Cascieri
Margaret A
MA
Yang
Lihu
L
D000284:Administration, Oral; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D002633:Chemotaxis; D004285:Dogs; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D008253:Macaca mulatta; D008956:Models, Chemical; D015394:Molecular Structure; D051381:Rats; D017207:Rats, Sprague-Dawley; D054390:Receptors, CCR2 / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D013329:Structure-Activity Relationship
D054390:Receptors, CCR2