Synthesis and preliminary biological studies of 4- and 5-[2-hydroxy-3-(isopropylamino)propoxy]benzimidazoles: selective β2 adrenergic blocking agents
- 1 February 1979
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 22 (2) , 210-214
- https://doi.org/10.1021/jm00188a019
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 .beta.2 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. .beta.2 selectivity of the C-5 isomer was minimal, with a potency about 1/100 that of propranolol.This publication has 0 references indexed in Scilit: