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

…, KS Gudmundsson, S Jenkinson, A Spaltenstein…

Index: Miller, John F.; Turner, Elizabeth M.; Gudmundsson, Kristjan S.; Jenkinson, Stephen; Spaltenstein, Andrew; Thomson, Michael; Wheelan, Pat Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 7 p. 2125 - 2128

Full Text: HTML

Citation Number: 43

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.