Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders

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 compound 22 showed efficacy in a cuprizone-in...

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Veröffentlicht in:	ACS medicinal chemistry letters 2016-04, Vol.7 (4), p.397-402
Hauptverfasser:	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
Format:	Artikel
Sprache:	eng
Schlagworte:	Letter
Online-Zugang:	Volltext
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