4-Oxospiro[benzopyran-2,4'-piperidines] as selective alpha 1a-adrenergic receptor antagonists |
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| 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 |
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| Institution: | Department of Medicinal Chemistry, Merck & Co., West Point, PA 19486, USA. |
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| Abstract: | The 4-oxospirobenzopyran-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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