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Synthesis and preliminary biological studies of 4- and 5-[2-hydroxy-3-(isopropylamino)propoxy]benzimidazoles: selective beta2 adrenergic blocking agents.

Abstract：

:Benzimidazoles carrying the 2-hydroxy-3-(isopropylamino)propoxy side chain at either the C-4 or C-5 ring positions were synthesized and investigated for beta-adrenergic blocking activity. Both compounds demonstrated beta2 selectivity when evaluated in guinea pig atrial and tracheal preparations. The C-4 isomer was 17 times more selective toward tracheal tissue, and its overall potency was roughly comparable to that of propranolol. beta2 selectivity of the C-5 isomer was minimal, with a potency about one-hundredth that of propranolol.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Crooks CR,Wright J,Callery PS,Moreton JE

doi

10.1021/jm00188a019

subject

Has Abstract

pub_date

1979-02-01 00:00:00

pages

210-4

issue

2

eissn

0022-2623

issn

1520-4804

journal_volume

22

pub_type

杂志文章

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