Brzozowski Z, Pomarnacka E, Oledzka K, Filczewski M
Department of Drug Technology, Medical University of Gdańsk, Poland.
Acta Pol Pharm. 1995 May-Jun;52(3):223-30.
The syntheses of salts [III, IV] and amides [V, V.HCl] of 2-[5-chloro-4-methyl-2-[(5-amino-s-triazol-3-yl)aminosulphonyl+ ++] phenylthio] alkanoic acids, as well as 5-amino-2-[2-(2,4-dimethylpiperidino) ethyl]-3-[4-chloro-2-[2-(2,6-dimethylpiperidino) ethylthio]-5-methylbenzenesulphonylimino]-1-methyl-delta 4-1,2,4-triazoline dihydrochloride [X] and 5-(amino-, 4-chloroanilino- or 3,4,5-trimethoxyanilino)-1,2-di[2-(2,6-dimethylpiperidino) ethyl]-3-(4-chloro-2-[2-(2,6-dimethylpiperidino) ethylthio]-5-methylbenzenesulphonylimino)-delta 4-1,2,4-triazoline trihydrochlorides [XI-XIII] are described. The results of preliminary pharmacological examinations such as acute toxicity and influence on circulatory system of compounds III, IV, V.HCl and X-XIII are presented. The antiarrhythmic effect of the most active [XI] was stronger or comparable to the reference drugs quinidine and procainamide.
描述了2-[5-氯-4-甲基-2-[(5-氨基-s-三唑-3-基)氨基磺酰基]苯硫基]链烷酸的盐[III, IV]和酰胺[V, V.HCl]，以及5-氨基-2-[2-(2,4-二甲基哌啶基)乙基]-3-[4-氯-2-[2-(2,6-二甲基哌啶基)乙硫基]-5-甲基苯磺酰亚氨基]-1-甲基-δ4-1,2,4-三唑啉二盐酸盐[X]和5-(氨基-、4-氯苯胺基-或3,4,5-三甲氧基苯胺基)-1,2-二[2-(2,6-二甲基哌啶基)乙基]-3-(4-氯-2-[2-(2,6-二甲基哌啶基)乙硫基]-5-甲基苯磺酰亚氨基)-δ4-1,2,4-三唑啉三盐酸盐[XI-XIII]的合成。给出了化合物III、IV、V.HCl和X-XIII的初步药理学研究结果，如急性毒性和对循环系统的影响。活性最强的化合物[XI]的抗心律失常作用比参考药物奎尼丁和普鲁卡因胺更强或相当。
