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.
Jee Woong Lim  1 ,  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
Affiliations
  • 1. Yangji Chemicals, Gyeonggi Bio-Center, Suwon 443-766, Republic of Korea. [email protected]
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.