Design and synthesis of N-alkylated saccharins as selective α-1a adrenergic receptor antagonists

JB Nerenberg, JM Erb, WJ Thompson, HY Lee…

Index: Nerenberg, Jennie B.; Erb, Jill M.; Thompson, Wayne J.; Lee, Hee-Yoon; Guare, James P.; Munson, Peter M.; Bergman, Jeffrey M.; Huff, Joel R.; Broten, Theodore P.; Chang, Raymond S. L.; Chen, Tsing B.; O'Malley, Stacey; Schorn, Terry W.; Scott, Ann L. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 18 p. 2467 - 2472

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Citation Number: 17

Abstract

Benign prostatic hyperplasia can be managed pharmacologically with α-1 adrenergic receptor antagonists. Agents that demonstrate selectivity for the α-1 a receptor subtype may offer advantages in clinical applications with respect to hypotensive side effects. The N- alkylated saccharins reported here represent a new class of subtype selective α-1 a adrenergic receptor antagonists which demonstrate potent effects on prostate function in ...

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