Journal of medicinal chemistry

Synthesis, saludiuretic, and antihypertensive activity of 6, 7-disubstituted 1 (2H)-and 3, 4-dihydro-1 (2H)-phthalazinones

S Cherkez, J Herzig, H Yellin

Index: Cherkez, S.; Herzig, J.; Yellin, H. Journal of Medicinal Chemistry, 1986 , vol. 29, # 6 p. 947 - 959

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Citation Number: 25

Abstract

The synthesis of the isomeric series 6-chloro-7-sulfamoyl-and 7-chloro-6-sulfamoyl-1 (2H)- phthalazinones (1 and 2) and 6-chloro-7-sulfamoyl-and 7-chloro-6-sulf~ oyl-3, 4-dihyd~ l (~- ph~ azinones (3 and 4), combining structural features characteristic to furosemide and hydralazine, is described, the mechanism of the formation of 1 and 2 is discussed, and their structure-activities relationships are studied. Preliminary screening in the rat shows that ...