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

doi:10.1021/acsmedchemlett.5b00489

	Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders
	Xu, Heng 2; Lu, Hongfu 1; Xu, Zhongmiao 1; Luan, Linbo 1; Li, Chengyong 1; Xu, Yan 1; Dong, Kelly 1; Zhang, Jinqiang 1; Li, Xiong 1; Li, Yvonne 1
刊名	ACS medicinal chemistry letters
	2016-04-14
卷号	7 期号:4 页码:397-402
ISSN号	1948-5875
DOI	10.1021/acsmedchemlett.5b00489
文献子类	Article
英文摘要	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-induced demyelination model with twice daily oral administration, thereby supporting CXCR2 to be a potential therapeutic target for the treatment of demyelinating diseases such as multiple sclerosis.
语种	英语
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/266595]
专题	中国科学院上海药物研究所
作者单位	1.Research and Development, GlaxoSmithKline , No. 3 Building, 898 Halei Road, Pudong, Shanghai 201203, P. R. China 2.State Key Laboratory of Bioactive Substances and Function of Natural Medicine, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences , 1 Xiannongtan Street, Beijing 100050, P. R. China;
推荐引用方式 GB/T 7714	Xu, Heng,Lu, Hongfu,Xu, Zhongmiao,et al. Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders[J]. ACS medicinal chemistry letters,2016,7(4):397-402.
APA	Xu, Heng.,Lu, Hongfu.,Xu, Zhongmiao.,Luan, Linbo.,Li, Chengyong.,...&Lin, Xichen.(2016).Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders.ACS medicinal chemistry letters,7(4),397-402.
MLA	Xu, Heng,et al."Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders".ACS medicinal chemistry letters 7.4(2016):397-402.