Structure-activity relationships of the diuretic activity of triaza- and tetraaza-naphthalene compounds.

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Abstract
The diuretic activity of 219 N containing heterocyclic compounds, classified into 13 groups based on the structural features, was studied on the saline loaded rats. Of the 219 compounds, 104 were active at the oral doses of 10-30 mg/kg. Several pyrimidopyridazines, pyridazinopyridazines and pyridopyridazines produced as potent diuresis and natriuresis as hydrochlorothiazide at the oral dose of 0.1 mg/kg, in which 2-phenyl-5,8-dimorpholinopyrimido[4,5-d]-pyridazine (DS-210) and 1,4-dimorpholino-7-phenylpyrido[3,4-d]pyridazine (DS-511) were selected for more extensive evaluation as diuretic agents. Structure-activity relationships of the tested compounds are discussed.

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