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[C-烷基哌嗪。十二。与氯噻嗪结构相关的化合物的合成及利尿活性]

[C-alkylpiperazines. XII. Synthesis and diuretic activity of compounds structurally related to clopamide].

作者信息

Landriani L, Barlocco D, Cignarella G, Curzu M M, Anania V, Desole M S

机构信息

Istituto Chimico Farmaceutico e Tossicologico, Università di Milano.

出版信息

Farmaco Sci. 1987 Mar;42(3):191-204.

PMID:3653386
Abstract

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.

摘要

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。

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