Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists

Jee Woong Lim; Youna Oh; Jong-Hoon Kim; Min-Ho Oak; Yongho Na; Jung-Ok Lee; Seung-Woo Lee; Heeyeong Cho; Woo-Kyu Park; Gildon Choi; Jongmin Kang

doi:10.1016/j.bmcl.2010.02.072

Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2099-102. doi: 10.1016/j.bmcl.2010.02.072. Epub 2010 Feb 20.

Authors

Jee Woong Lim¹, Youna Oh, Jong-Hoon Kim, Min-Ho Oak, Yongho Na, Jung-Ok Lee, Seung-Woo Lee, Heeyeong Cho, Woo-Kyu Park, Gildon Choi, Jongmin Kang

Affiliation

¹ Yangji Chemicals, Gyeonggi Bio-Center, Suwon 443-766, Republic of Korea. [email protected]

PMID: 20223662
DOI: 10.1016/j.bmcl.2010.02.072

Abstract

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.

MeSH terms

Cell Line
Chemotaxis / drug effects
Humans
Inhibitory Concentration 50
Protein Binding / drug effects
Pyrrolidines / chemical synthesis
Pyrrolidines / chemistry*
Pyrrolidines / pharmacology*
Receptors, CCR2 / antagonists & inhibitors*
Receptors, CCR2 / metabolism*
Structure-Activity Relationship

Substances

Pyrrolidines
Receptors, CCR2