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.

Graphical abstract3-Aminopyrrolidine derivatives were synthesized and evaluated as potent chemokine receptor 2 (CCR2) antagonists.Figure optionsDownload full-size imageDownload as PowerPoint slide