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

@article{Shao2011IISS,
  title={II. SAR studies of pyridyl-piperazinyl-piperidine derivatives as CXCR3 chemokine antagonists.},
  author={Yuefei Shao and Gopinadhan N Anilkumar and Carolyn Diianni Carroll and Guizhen Dong and James W. Hall and Doug W. Hobbs and Yueheng Jiang and C H Jenh and Seong Heon Kim and Joseph A Kozlowski and Brian F McGuinness and Stuart B Rosenblum and Inna Schulman and Neng-Yang Shih and Youheng Shu and Michael Kwok Wong and Wensheng Yu and Lisa Guise Zawacki and Qingbei Zeng},
  journal={Bioorganic & medicinal chemistry letters},
  year={2011},
  volume={21 5},
  pages={1527-31}
}
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 IC(50) of 0.2 nM. 

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