Substituted pyrrolidin-2-one biphenyltetrazoles as angiotensin II antagonists

Abstract A novel series of substituted pyrrolidin-2-ones has been identified as antagonists of the angiotensin II receptor. They are potent inhibitors of angiotensin II induced contractions in rabbit aortic rings, with pA 2 values as high as 9. A number of these compounds have been tested in rabbit adrenal cortex binding assays and exhibited IC 50 's as low as 60nM. Compounds 1e , 1f and 2e have been found to be orally active as anti-hypertensives in spontaneously hypertensive rat preparations.