3-SUBSTITUTED 6-BUTYL-1,2-DIHYDROPYRIDIN-2-ONES - A NEW SERIES OF POTENT NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS

The syntheses and biological activities of a series of novel 3-substituted 6-butyl-1,2-dihyro-pyridin-2-ones are presented. A number of these compounds are shown to be potent antagonists of angiotensin II with in vitro potencies in the nanomolar or even subnanomolar range. They also have proven their suitability as effective inhibitors of angiotensin II pressor response in vivo.