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Substituted piperidin-2-one biphenyltetrazoles as angiotensin II antagonists |
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| Authors: | W. V. Murray P. Lalan A. Gill M. F. Addo J. M. Lewis D. K. H. Lee R. Rampulla M. P. Wachter J. D. Hsi D. C. Underwood |
| Affiliation: | The R.W. Johnson Pharmaceutical Research Institute, P.O. Box 300, Route 202, Raritan, New Jersey 08869 USA |
| 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. |
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