Novel N-substituted benzimidazole CXCR4 antagonists as potential anti-HIV agents
John F Miller1, Elizabeth M Turner, Kristjan S Gudmundsson
1Department 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. john.6.miller@gsk.com
Bioorganic & Medicinal Chemistry Letters
|March 9, 2010
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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