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

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Abstract—

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.

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Authors and Affiliations

  1. Danylo Halytsky Lviv National Medical University, 79010, Lviv, Ukraine

    V. Ya. Horishny

  2. Ivan Franko National University of Lviv, 79005, Lviv, Ukraine

    V. S. Matiychuk

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  1. V. Ya. Horishny
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  2. V. S. Matiychuk
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Correspondence to V. S. Matiychuk.

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The paper does not contain any studies involving animal or human participants performed by any of the authors.

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Translated by S. Sidorova

Abbreviations: MIC, minimum inhibitory concentration.

Corresponding author: (phone: +38 (067) 675-16-83).

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Horishny, V.Y., Matiychuk, V.S. Synthesis, Antimicrobial and Antitumor Properties of 5-Thiophen-2-ylmethylen-2-Thioxothiazolidin-4-one Derivatives. Russ J Bioorg Chem 47, 749–756 (2021). https://doi.org/10.1134/S1068162021030079

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