PMID: 37337Jun 1, 1979

beta-Adrenergic blocking agents with acute antihypertensive activity

Journal of Medicinal Chemistry
J J BaldwinR Hall

Abstract

Modification of the pharmacological profile of the vasodilating/beta-adrenergic blocking agent 2-[4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl]-4-(trifluoromethyl)imidazole (1) has been investigated. Introduction of selected substitutents onto the imidazole ring, in place of the trifluoromethyl group, has yielded highly cardioselective beta-adrenergic blocking agents such as 7, 17, and 18. The placement of alkyl or chloro groups onto the aryl ring of 1, as illustrated by 33, has produced a class of compounds characterized as antihypertensive beta-adrenergic blocking agents. In these examples, the acute antihypertensive activity does not appear to be due to either vasodilating or beta 2-agonist properties.

Citations

Feb 8, 1980·European Journal of Pharmacology·D DeitchmanR W Snyder
May 31, 2012·Journal of the American Chemical Society·Adam S DuerfeldtBrian S J Blagg

Related Concepts

Adrenergic beta-Antagonists
Airway Resistance
Antihypertensive Agents
Diastolic Blood Pressure
Canis familiaris
Heart
Pulse Rate
Hypertensive Disease
Structure of Iliac Artery
Imidazoles

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