Synthesis, Antimicrobial and Antitumor Properties of 5-Thiophen-2-ylmethylen-2-Thioxothiazolidin-4-one Derivatives

被引：0

作者：

Horishny, V. Ya ^{[1
]}

Matiychuk, V. S. ^{[2
]}

机构：

[1] Danylo Halytsky Lviv Natl Med Univ, UA-79010 Lvov, Ukraine

[2] Ivan Franko Natl Univ Lviv, UA-79005 Lvov, Ukraine

来源：

RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY | 2021年 / 47卷 / 03期

关键词：

thiophene; rhodanine; acylation; antimicrobial activity; antitumor activity; BIOLOGICAL EVALUATION; SELECTIVE INHIBITORS; RHODANINE; DISCOVERY; SCAFFOLD; POTENT;

D O I：

10.1134/S1068162021030079

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

By the reaction of thiophen-2-carbaldehyde with rhodanine derivatives, 5-thiophen-2-ylmethylene-2-thioxothiazolidin-4-ones have been synthesized. The resulting (4-oxo-5-thiophen-2-ylmethylen-2-thioxothiazolidin-3-yl)alkane carboxylic acids have been used to acylate the biogenic amine tryptamine and its derivatives. As a result, a number of novel N-[2-(5-[R-1H-indol-3-yl)-ethyl]-2-(4-oxo-5-thiophen-2-ylmethylen-2-thioxothiazolidin-3-yl)carbamides have been synthesized. The antimicrobial and antitumor properties of the resulting compounds have been tested. Compounds with a high antimicrobial activity against Staphylococcus aureus and Cryptococcus neoformans have been identified.

引用

页码：749 / 756

页数：8

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