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[乙胺碘呋酮类似物的化学结构与抗心律失常作用之间的关系]

[Relationship between chemical structure and anti-arrhythmic effect of ethmosine analogs].

作者信息

Senova Z P, Lyskovtsev V V

出版信息

Farmakol Toksikol. 1976 May-Jun;39(3):293-6.

PMID:1026511
Abstract

The relationship between the chemical structure and antiarrhthmic action in the series of 10-actlaminopropionyl phenothiazine derivatives with different urethan groups in the second position of the phenothiazine cycle (methy, ethyl and isobutyl) was studied. Subject to investigation were also aetmozine isomers containing ethyl-carbaminate in the first, third and fourth position, as well as compounds containing aminopropionyl residues in the tenth and trifluoromethyl group or bromine in the second position. The available data indicated that the antiarrhythmic action of 10-acylamino-derivatives of phenothiazine depends not only on the structure of the side chain and substitution of hydrogen in the second position of the phenothiazine nucleus, but also upon the position of the urethan group in the phenothiazine cycle. Moving ethyl-carbaminate to the first, third and fourth positions results in the fall of the anti-arrhythmic action. The absence of any relation between the length of the urethan radical and the effect produced by the substance was also shown. By substituting the methyl or isobutyl radicals for the ethyl one the antiarrthythmic action of the substances declines.

摘要

研究了在吩噻嗪环第二位带有不同氨基甲酸酯基团(甲基、乙基和异丁基)的一系列10-氨基丙酰基吩噻嗪衍生物的化学结构与抗心律失常作用之间的关系。还对在第一、第三和第四位含有乙基氨基甲酸酯的乙胺嗪异构体,以及在第十位含有氨基丙酰基残基且在第二位含有三氟甲基或溴的化合物进行了研究。现有数据表明,吩噻嗪的10-酰基氨基衍生物的抗心律失常作用不仅取决于侧链结构和吩噻嗪核第二位氢的取代情况,还取决于氨基甲酸酯基团在吩噻嗪环中的位置。将乙基氨基甲酸酯移至第一、第三和第四位会导致抗心律失常作用减弱。还表明氨基甲酸酯基团的长度与该物质产生的效应之间不存在任何关系。用甲基或异丁基取代乙基会使这些物质的抗心律失常作用降低。

相似文献

3
[Mechanism of the antiarrhythmic action of etmozin].
Farmakol Toksikol. 1973;36(5):703-6.
10
[Pharmacology of ethmosine].
Farmakol Toksikol. 1972 Mar-Apr;35(2):182-5.

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