Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists.
Novel 3-aminopyrrolidine derivatives were synthesized and evaluated for their antagonistic activity against human chemokine receptor 2. Structure-activity studies on 3-aminopyrrolidine incorporating heteroatomic carbocycle moieties led to piperidine compound 19, and piperazine compounds 42, 47 and 49 as highly potent hCCR2 antagonists.
Lim
Jee Woong
JW
Yangji Chemicals, Gyeonggi Bio-Center, Suwon 443-766, Republic of Korea. srhnys@hwpharm.com
Oh
Youna
Y
Kim
Jong-Hoon
JH
Oak
Min-Ho
MH
Na
Yongho
Y
Lee
Jung-Ok
JO
Lee
Seung-Woo
SW
Cho
Heeyeong
H
Park
Woo-Kyu
WK
Choi
Gildon
G
Kang
Jongmin
J
D002460:Cell Line; D002633:Chemotaxis / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D011485:Protein Binding / Q000187:drug effects; D011759:Pyrrolidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D054390:Receptors, CCR2 / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D013329:Structure-Activity Relationship
D011759:Pyrrolidines; D054390:Receptors, CCR2