Synthesis and Cardiotropic Activity of N,N′-Diarylpropane-1,3-Diamines

被引:0
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作者
G. V. Mokrov
T. Yu. Vorob’eva
V. E. Biryukova
E. I. Barchukova
V. V. Barchukov
I. B. Tsorin
M. B. Vititnova
A. G. Rebeko
S. A. Kryzhanovskii
机构
[1] V. V. Zakusov Science Research Institute of Pharmacology,
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关键词
anti-ischemic and antiarrhythmic activity; biaromatic compounds; multitarget cardioprotectors;
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摘要
We report here the synthesis of novel compounds of the bis-(2,3,4-trimethoxybenzyl)propanediamines group and studies of their anti-ischemic and antiarrhythmic activity. Introduction of a hydroxyl group into the central part of the propane linker was found to produce virtually no change in the spectrum of cardiotropic properties of the unsubstituted compound ALM-851, while introduction of two methyl groups led to the complete disappearance of both antiarrhythmic and antiischemic activities. Compound ALM-850 (1,3-bis((2,3,4-trimethoxy-benzyl)amino)propan-2-oldihydrochloride) at a dose of 3 mg/kg significantly blocked the development of rhythm disturbances and death in animals in the aconitine and calcium chloride arrhythmia models, and also decreased ST segment depression in the isoproterenol ischemia model.
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页码:975 / 980
页数:5
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