期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 7, 页码 2125-2128出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.02.053
关键词
CXCR4; Benzimidazole; Tetrahydroquinoline; HIV; Antiviral
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. (C) 2010 Elsevier Ltd. All rights reserved.
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