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Angiotensin converting enzyme inhibitors. 9. Novel [[N-(1-carboxyl-3-phenylpropyl)amino]acyl]glycine derivatives with diuretic activity
Journal of Medicinal Chemistry1990Vol. 33(6), pp. 1600–1606
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J Barton, John J. Piwinski, Jerry W. Skiles, John R. Regan, Paul R. Menard, Rohit Desai, F. S. Golec, Laurence W. Reilly, Thomas Goetzen
Abstract
A series of molecules 1 having sulfonamide diuretic moieties covalently linked to non-sulfhydryl angiotensin-converting enzyme inhibitors (ACEI) were prepared and tested for both activities. IC50 values for ACEI as low as 7 nM were observed. Discernable diuretic activity was seen for several hydrochlorothiazide-based molecules. Effects of the ACEI and diuretic structures on the respective potencies are discussed.
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