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4-Oxospiro[benzopyran-2,4'-piperidines] as selective alpha 1a-adrenergic receptor antagonists
Authors:Nerenberg J B  Erb J M  Bergman J M  O'Malley S  Chang R S  Scott A L  Broten T P  Bock M G
Affiliation:Department of Medicinal Chemistry, Merck & Co., West Point, PA 19486, USA.
Abstract:The 4-oxospiro[benzopyran-2,4'-piperidine] ring system is contained within potent class III antiarrhythmic agents. We highlight how these agents can be chemically transformed into a new class of potent (< 1 nM) and selective (> 25-fold) alpha 1a-receptor subtype adrenergic antagonists.
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