Design, Synthesis, and Cardiotropic Properties of N1-Benzyl-N2-{2-[(2,3,4-Trimethoxybenzyl)Amino]-Ethyl}Ethane-1,2-Diamines

被引:0
|
作者
Mokrov, G. V. [1 ]
Vorobieva, T. Yu. [1 ]
Birukova, V. E. [1 ]
Pantileev, A. S. [1 ]
Barchukova, E. I. [1 ]
Tsorin, I. B. [1 ]
Vititnova, M. B. [1 ]
Rebeko, A. G. [1 ]
Kryzhanovskiy, S. A. [1 ]
Gudasheva, T. A. [1 ]
Dorofeev, V. L. [1 ]
机构
[1] Fed Res Ctr Innovator & Emerging Biomed & Pharmace, 8 Baltiiskaya St, Moscow 125315, Russia
关键词
anti-ischemic activity; antiarrhythmic activity; biaromatic compounds; multitarget cardioprotective agents; ALM-802;
D O I
10.1007/s11094-024-03198-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A new group of unsymmetrical ALM-802 analogs, N-1-benzyl-N-2-{2-[(2,3,4-trimethoxybenzyl)amino]-ethyl}ethane-1,2-diamines of general formula 1, in which one of the aromatic groups was changed, was studied. The anti-ischemic and antiarrhythmic activities of the new compounds were studied. Their ADME characteristics were analyzed. The 2,3,4-trimethoxyphenyl group used as one of the aromatic pharmacophores was shown to play a key role in the activity of compounds of this type. The presence of a second aromatic group was also important since its removal led to the disappearance of cardiotropic activity. However, its structure had significantly less impact on the activity of the corresponding compounds because a rather wide variation of substituents in this group did not change the activity in most arrhythmia and ischemia models.
引用
收藏
页码:715 / 725
页数:11
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