M. Osswald et al., 3-SUBSTITUTED 6-BUTYL-1,2-DIHYDROPYRIDIN-2-ONES - A NEW SERIES OF POTENT NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 4(5), 1994, pp. 683-688
The syntheses and biological activities of a series of novel 3-substit
uted 6-butyl-1,2-dihyro-pyridin-2-ones are presented. A number of thes
e compounds are shown to be potent antagonists of angiotensin II with
in vitro potencies in the nanomolar or even subnanomolar range. They a
lso have proven their suitability as effective inhibitors of angiotens
in II pressor response in vivo.