New 5H-[1,3]thiazolo[3,2-a]pyrido[3,2-e]pyrimidine derivatives as diuretics

New 5H-1,3]thiazolo3,2-a]pyrido3,2-e]pyrimidines 1 and 6,10-dihydro-5H-pyrido3',2':5,6]pyrimido2,1-c] 1,2,4]triazines 4 with 5-one, 5-thione or 5-hydrazono substituents and in some cases 1,2,3,4 or 8,9 hydrogenated are synthetized. The diuretic, natriuretic and kaliuretic activities of these compounds in Wistar rats at a dose of 24 mg/kg were estimated. A series of 24 possible derivatives of 1 and 4 possessing diuretic and saliuretic activities are investigated for structure-activity relationships in light of Fujita-Ban model. The Fujita-Ban group contributions have been calculated for different structural variations on the parent ring 1a. It is observed that the hydrogenation of pyridine, 1,3]thiazole or 1,2,4]triazine rings on 1 or 4 decrease the diuretic and saliuretic activities.