Identification and SAR around N-{2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide, a selective alpha2C adrenergic receptor antagonist

The discovery of the CNS-penetrant and selective alpha(2C) adrenergic receptor antagonist N-{2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide, 13 is described. Structure-activity studies demonstrate the structural requirements for binding affinity, fun...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2008-10, Vol.18 (20), p.5689-5693
Hauptverfasser:	Patel, Snahel D, Habeski, Wendy M, Min, Hyunsuk, Zhang, Jiansu, Roof, Robin, Snyder, Bradley, Bora, Gary, Campbell, Brian, Li, Cheryl, Hidayetoglu, Debra, Johnson, Douglas S, Chaudhry, Archana, Charlton, Maura E, Kablaoui, Natasha M
Format:	Artikel
Sprache:	eng
Schlagworte:	Adrenergic alpha-2 Receptor Antagonists Animals Azepines - chemical synthesis Azepines - pharmacology Brain - metabolism Central Nervous System - drug effects Cerebrospinal Fluid - metabolism Chemistry, Pharmaceutical - methods Drug Design Humans Kinetics Male Molecular Conformation Niacinamide - analogs & derivatives Niacinamide - chemical synthesis Niacinamide - pharmacology Rats Rats, Inbred WKY Receptors, Adrenergic, alpha-2 - chemistry Structure-Activity Relationship
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Zusammenfassung:	The discovery of the CNS-penetrant and selective alpha(2C) adrenergic receptor antagonist N-{2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide, 13 is described. Structure-activity studies demonstrate the structural requirements for binding affinity, functional activity, and selectivity over other alpha(2)-AR subtypes.
ISSN:	1464-3405
DOI:	10.1016/j.bmcl.2008.08.055