Key result
Novel nitrogen-containing heterocyclic compounds demonstrated angiotensin II antagonist properties in animal models, with a specified compound showing an IC50 of 3.48 × 10−9M for AII binding.
Novel nitrogen-containing heterocycles demonstrate potent angiotensin II antagonist properties in preclinical models, suggesting potential utility for hypertension and congestive heart failure.
Hypothesis-generating for novel AII antagonists; leaves open translation to human hypertension or heart failure therapy.
SummaryNovelty: Novel nitrogeneous heterocyclic compounds are disclosed as antagonists of one or more of the actions of angiotensins. They may be used to treat hypertension and congestive heart failure.Biology: The angiotensin II (AII) antagonist properties were assayed in standard tests: displacement of AII binding in guinea pig adrenal gland membranes, antagonism of AII-induced contraction of isolated rabbit aorta, antagonism of AII-induced pressor responses in terminally anaesthetized or conscious rats, and stimulation of endogenous AII biosynthesis in rat, marmoset and dog on a low sodium diet given daily doses of frusemide. The specified compound gave an IC50 of 3.48 × 10−9M in the first test and an ED50 of 0.047 mg/kg in iv in the third.Chemistry: Sixteen examples are given of the preparation of the compounds by standard techniques. 2,6-Dimethyl-3-iodo-4-[(2'-(1H-tetrazol-5-yl)biphenyld-yl)methylamino]pyridine is an exemplified compound. None of the compounds is specifically claimed.
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A 1992 study studied Hypertension and congestive heart failure. Nitrogen-containing heterocycles was evaluated on Angiotensin II binding displacement and antagonism of AII-induced responses. Novel nitrogen-containing heterocyclic compounds demonstrated angiotensin II antagonist properties in animal models, with a specified compound showing an IC50 of 3.48 × 10−9M for AII binding.
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