906806-16-4Relevant articles and documents
III. Identification of novel CXCR3 chemokine receptor antagonists with a pyrazinyl-piperazinyl-piperidine scaffold
Kim, Seong Heon,Anilkumar, Gopinadhan N.,Zawacki, Lisa Guise,Zeng, Qingbei,Yang, De-Yi,Shao, Yuefei,Dong, Guizhen,Xu, Xiaolian,Yu, Wensheng,Jiang, Yueheng,Jenh, Chung-Her,Hall III, James W.,Carroll, Carolyn Diianni,Hobbs, Doug W.,Baldwin, John J.,McGuinness, Brian F.,Rosenblum, Stuart B.,Kozlowski, Joseph A.,Shankar, Bandarpalle B.,Shih, Neng-Yang
, p. 6982 - 6986 (2011)
The SAR of a novel pyrazinyl-piperazinyl-piperidine scaffold with CXCR3 receptor antagonist activity was explored. Optimization of the DMPK profile and reduction of hERG inhibition is described. Compound 16e with single-digit CXCR3 affinity, good rat PK a