Synthesis and in vitro evaluation of derivatives of the β 1-adrenergic receptor antagonist HX-CH 44

KA Stephenson, AA Wilson, S Houle…

Index: Stephenson, Karin A.; Wilson, Alan A.; Houle, Sylvain; Vasdev, Neil Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 18 p. 5506 - 5509

Full Text: HTML

Citation Number: 7

Abstract

Isopropyl-and fluoroisopropyl-amino derivatives of the β1-adrenergic receptor antagonist 2- [4-[3-(tert-butyl-amino)-2-hydroxypropoxy] phenyl]-3-methyl-6-methoxy-4 (3H)- quinazolinone ((±) HX-CH 44) were synthesized, including a concise and efficient preparation of the core, 2-(4-hydroxyphenyl)-6-methoxy-3-methylquinazolin-4 (3H)-one. In vitro binding assays showed that the fluorinated analog was selective towards β1- ...