Substituted piperidin-2-one biphenyltetrazoles as angiotensin II antagonists

doi:10.1016/S0960-894X(00)80474-6

Bioorganic & Medicinal Chemistry Letters

Volume 2, Issue 12, December 1992, Pages 1775-1779

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Abstract

A novel series of substituted piperidine-2-ones has been identified as antagonists of angiotensin II. These compounds showed high affinity for the receptor in bovine adrenal cortex binding assays with IC₅₀'s as low as 20nM. They are potent inhibitors of angiotensin II induced contractions in rabbit aortic rings, with pA₂ values as high as 9. A number of these compounds are also orally active as antihypertensives in spontaneously hypertensive rat preparations.

A novel series of piperidine-2-ones have been identified as antagonists of angiotensin II. These compounds are potent in bovie adrenal cortex binding assays with IC₅₀'s as low as 20nM. They also show pA₂'s of up to 9 in rabbit aortic ring assays. A number of these compounds are also orally active as antihypertensives in spontaneously hypertensive rat preparations.

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Substituted piperidin-2-one biphenyltetrazoles as angiotensin II antagonists

Abstract

Biochem. Pharmacol.

Can J. Chem.

Jpn. Circl. J.

Science

J. Med. Chem.

Nature

J. Med. Chem.

J. Med. Chem.

J. Med. Chem.

J. Med. Chem.

Bioorg. Med. Chem. Lett.

Trends Pharmacol. Sci.