1279723-87-3Relevant academic research and scientific papers
II. SAR studies of pyridyl-piperazinyl-piperidine derivatives as CXCR3 chemokine antagonists
Shao, Yuefei,Anilkumar, Gopinadhan N.,Carroll, Carolyn Diianni,Dong, Guizhen,Hall III, James W.,Hobbs, Doug W.,Jiang, Yueheng,Jenh, Chung-Her,Kim, Seong Heon,Kozlowski, Joseph A.,McGuinness, Brian F.,Rosenblum, Stuart B.,Schulman, Inna,Shih, Neng-Yang,Shu, Youheng,Wong, Michael K.C.,Yu, Wensheng,Zawacki, Lisa Guise,Zeng, Qingbei
, p. 1527 - 1531 (2011/04/16)
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.
