
Bioorganic and Medicinal Chemistry Letters p. 6982 - 6986 (2011)
Update date:2022-08-04
Topics:
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
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
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Doi:10.1021/ja01015a021
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