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

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Abstract

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.

Graphical abstract

The structure–human CXCR3 binding affinity relationship of a series of pyridyl–piperazinyl-piperidine derivatives was explored.

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