Indoloxypropanolamine analogues as 5-HT 1A receptor antagonists

JH Krushinski, JM Schaus, DC Thompson…

Index: Krushinski Jr., Joseph H.; Schaus, John M.; Thompson, Dennis C.; Calligaro, David O.; Nelson, David L.; Luecke, Susan H.; Wainscott, David B.; Wong, David T. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 20 p. 5600 - 5604

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Citation Number: 6

Abstract

Analogues of pindolol, 1-(1H-indol-4-yloxy)-3-isopropylamino-propan-2-ol, were synthesized and evaluated as 5-HT1A receptor antagonists. The structural features required for optimal binding to the 5-HT1A receptor are as follows: S-2-propanol linker, 4-indoloxy substituent, and a large lipophilic cyclic amine substituent.