201467-03-0Relevant articles and documents
Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders
Xu, Heng,Lu, Hongfu,Xu, Zhongmiao,Luan, Linbo,Li, Chengyong,Xu, Yan,Dong, Kelly,Zhang, Jinqiang,Li, Xiong,Li, Yvonne,Liu, Gentao,Gong, Sophie,Zhao, Yong-Gang,Liu, Ailian,Zhang, Yueting,Zhang, Wei,Cai, Xin,Xiang, Jia-Ning,Elliott, John D.,Lin, Xichen
supporting information, p. 397 - 402 (2016/05/19)
Structure-activity relationship exploration of the historical biarylurea series led to the identification of novel CNS penetrant CXCR2 antagonists with nanomolar potency, favorable PK profile, and good developability potentials. More importantly, the key
Evaluation of Potent and Selective Small-Molecule Antagonists for the CXCR2 Chemokine Receptor
Widdowson, Katherine L.,Elliott, John D.,Veber, Daniel F.,Nie, Hong,Rutledge, Melvin C.,McCleland, Brent W.,Xiang, Jia-Ning,Jurewicz, Anthony J.,Hertzberg, Robert P.,Foley, James J.,Griswold, Don E.,Martin, Lenox,Lee, Judithann M.,White, John R.,Sarau, Henry M.
, p. 1319 - 1321 (2007/10/03)
N,N′-Diarylureas were prepared, and the structure-activity relationship relative to the CXCR2 receptor was examined. This led to the identification of a potent and highly selective CXCR2 antagonist, which in addition was shown to be functionally active bo
