Landriani L, Barlocco D, Cignarella G, Curzu M M, Anania V, Desole M S
Istituto Chimico Farmaceutico e Tossicologico, Università di Milano.
Farmaco Sci. 1987 Mar;42(3):191-204.
The synthesis and diuretic activity were reported of a series of N1-(4-chloro-3-sulfamoylbenzamide)-N4-alkylpiperazines, 2-methyl- and cis-2,6-dimethyl substituted, structurally related to clopamide, as well as of two N4-alkyl-N1-(4-chloro-3-sulfamoylbenzoyl)-2-methyl-1,2,3, 4-tetrahydroquinoxalines. In the piperazine series the presence of methyl group in position 2 and 6 of the piperazinic ring was found to increase the diuretic potency of the C-unmethylated compound.
报道了一系列N1-(4-氯-3-氨磺酰基苯甲酰胺)-N4-烷基哌嗪、2-甲基和顺式-2,6-二甲基取代物(其结构与氯哌酰胺相关)以及两种N4-烷基-N1-(4-氯-3-氨磺酰基苯甲酰基)-2-甲基-1,2,3,4-四氢喹喔啉的合成及利尿活性。在哌嗪系列中,发现哌嗪环2位和6位存在甲基会提高未甲基化的C化合物的利尿效力。