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
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
收藏
页码:749 / 756
页数:8
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