Novel N-substituted benzimidazole CXCR4 antagonists as potential anti-HIV agents期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

Novel N-substituted benzimidazole CXCR4 antagonists as potential anti-HIV agents

Authors:	John F. Miller Elizabeth M. Turner Kristjan S. Gudmundsson Stephen Jenkinson Andrew Spaltenstein Michael Thomson Pat Wheelan

Affiliation:	1. Department of Medicinal Chemistry, Infectious Diseases Center for Excellence in Drug Discovery, GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA;2. Department of Virology, Infectious Diseases Center for Excellence in Drug Discovery, GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA;3. Department of DMPK, Infectious Diseases Center for Excellence in Drug Discovery, GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA;4. Department of Biochemical and Analytical Pharmacology, Infectious Diseases Center for Excellence in Drug Discovery, GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA

Abstract:	The lead optimization of a series of N-substituted benzimidazole CXCR4 antagonists is described. Side chain modifications and stereochemical optimization led to substantial improvements in potency and protein shift to afford compounds with low nanomolar anti-HIV activity.

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