II. SAR studies of pyridyl–piperazinyl-piperidine derivatives as CXCR3 chemokine antagonists

The structure–human CXCR3 binding affinity relationship of a series of pyridyl–piperazinyl-piperidine derivatives was explored. The optimization campaign highlighted the pronounced effect of 2′-piperazine substitution on CXCR3 receptor affinity. Analog 18j, harboring a 2′(S)-ethylpiperazine moiety, exhibited a human CXCR3 IC50 of 0.2 nM.

The structure–human CXCR3 binding affinity relationship of a series of pyridyl–piperazinyl-piperidine derivatives was explored.Figure optionsDownload as PowerPoint slide