Phenylacetamides as selective alpha-1A adrenergic receptor antagonists

A novel class of potent and selective alpha-1a receptor antagonists has been identified. The structures of these antagonists were derived from truncating the 4-aryl dihydropyridine subunit present in known alpha-1a antagonists. The design principles which led to the discovery of substituted phenylac...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 10; no. 15; pp. 1621 - 1624
Main Authors:	Patane, M A, DiPardo, R M, Newton, R C, Price, R P, Broten, T P, Chang, R S, Ransom, R W, Di Salvo, J, Nagarathnam, D, Forray, C, Gluchowski, C, Bock, M G
Format:	Journal Article
Language:	English
Published:	England 07-08-2000
Subjects:	Acetamides - chemistry Acetamides - pharmacokinetics Acetamides - pharmacology Adrenergic alpha-1 Receptor Antagonists Adrenergic alpha-Antagonists - chemistry Adrenergic alpha-Antagonists - pharmacokinetics Adrenergic alpha-Antagonists - pharmacology Animals Chromatography, High Pressure Liquid Dogs Structure-Activity Relationship
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Summary:	A novel class of potent and selective alpha-1a receptor antagonists has been identified. The structures of these antagonists were derived from truncating the 4-aryl dihydropyridine subunit present in known alpha-1a antagonists. The design principles which led to the discovery of substituted phenylacetamides, the synthesis and SAR of key analogues, and the results of select in vitro and in vivo studies are described.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X
DOI:	10.1016/S0960-894X(00)00307-3