Novel heterocycles as selective alpha1-adrenergic receptor antagonists

A novel series of aryl piperazine substituted heterocycles has been synthesized and identified as antagonists of the alpha1a-adrenergic receptor (alpha1a-AR), which has been implicated in benign prostatic hyperplasia (BPH). These compounds selectively inhibit binding to the alpha1a-AR with K(i)s as...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-10, Vol.10 (20), p.2375-2377
Hauptverfasser:	Li, X, McCoy, K A, Murray, W V, Jolliffe, L, Pulito, V
Format:	Artikel
Sprache:	eng
Schlagworte:	Adrenergic alpha-1 Receptor Antagonists Adrenergic alpha-Antagonists - chemical synthesis Adrenergic alpha-Antagonists - chemistry Adrenergic alpha-Antagonists - pharmacology Animals Cell Membrane - physiology COS Cells Drug Design Heterocyclic Compounds - chemical synthesis Heterocyclic Compounds - chemistry Heterocyclic Compounds - pharmacology Humans Kinetics Male Prostatic Hyperplasia - physiopathology Receptors, Adrenergic, alpha-1 Recombinant Proteins - antagonists & inhibitors Structure-Activity Relationship Transfection
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Zusammenfassung:	A novel series of aryl piperazine substituted heterocycles has been synthesized and identified as antagonists of the alpha1a-adrenergic receptor (alpha1a-AR), which has been implicated in benign prostatic hyperplasia (BPH). These compounds selectively inhibit binding to the alpha1a-AR with K(i)s as low as 2.1 nM.
ISSN:	0960-894X