L-162393

The structure activity relationships of a series of 2-alkyl-6-(acylamino)-3-[((2'-acylaminosulfonyl)biphenyl-4-yl)methyl]quinazolin-4-(3H)-ones were studied to identify balanced angiotensin II antagonists capable of potent binding to both AT₁ and AT₂ angiotensin receptor subtypes.The optimization of the substitution pattern led to the discovery of a potent, balanced quinazolinone antagonist L-162,393, which displayed long lasting blockade of angiotensin pressor response in rats, dogs and rhesus monkeys.