Bioisosteric phentolamine analogs as potent α-adrenergic antagonists

…, PN Patil, SG Lalchandani, DR Feller, DD Miller

Index: Hong, Seoung-Soo; Bavadekar, Supriya A.; Lee, Sang-Il; Patil, Popat. N.; Lalchandani; Feller, Dennis R.; Miller, Duane D. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 21 p. 4691 - 4695

Full Text: HTML

Citation Number: 17

Abstract

The synthesis and biological evaluation of a new series of bioisosteric phentolamine analogs are described. Replacement of the carbon next to the imidazoline ring of phentolamine with a nitrogen atom provides compounds (2, 3) that are about 1.6 times and 4.1 times more potent functionally than phentolamine on rat α1-adrenergic receptors, respectively. In receptor binding assays, the affinities of phentolamine and its bioisosteric ...