Antihypertensive, Congestive Heart Failure/Angiotensin II Antagonist: A Potentially useful New Class of Angiotensin II Antagonists with Quinazolinone ‘Head’ Groups

Summary

Novelty: Novel substituted quinazolinones possessing angiotensin II (AII) antagonistic activity and useful as antihypertensive agents are disclosed. The compounds are also useful for treating congestive heart failure and in the treatment of elevated intraocular pressure.

Biology: Protocols for a receptor binding assay using a rabbit aorta membrane preparation and a bovine adrenal cortex preparation for determining AII antagonist activity are described, together with in vivo methods for evaluating antihypertensive effects in rats. Representative compounds exhibited IC₅₀ values of less than 50 μM.

Chemistry: 2-Butyl-6-methyl-3-[(2′-(tetrazol-5-yl)biphenyl-4-yl)methyl]quinazolin-4(3H)-one is one of ninety-nine exemplified compounds.