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

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. The lead optimization of a...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-04, Vol.20 (7), p.2125-2128
Hauptverfasser:	Miller, John F., Turner, Elizabeth M., Gudmundsson, Kristjan S., Jenkinson, Stephen, Spaltenstein, Andrew, Thomson, Michael, Wheelan, Pat
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-HIV Agents - chemistry Anti-HIV Agents - pharmacology Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral Antiviral agents Benzimidazole Benzimidazoles - chemistry Benzimidazoles - pharmacology Biological and medical sciences Cell Line CXCR4 HIV HIV Infections - drug therapy HIV-1 - drug effects Human immunodeficiency virus Humans Inhibitory Concentration 50 Medical sciences Pharmacology. Drug treatments Receptors, CXCR4 - antagonists & inhibitors Receptors, CXCR4 - metabolism Tetrahydroquinoline
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Zusammenfassung:	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. 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2010.02.053