SYNTHESIS AND BIOLOGICAL ACTIVITY EVALUATION OF 5-INDOLIDENERHODANINES
DOI:
https://doi.org/10.11603/2312-0967.2024.4.15010Keywords:
indole, thiazolidinones, antimicrobial activity, cytotoxicityAbstract
The aim of the work - to synthesize 5-inolidenerhodanines and investigate their anticancer activity and cytotoxicity.
Materials and Methods. During the research, organic synthesis methods were used, and physicochemical analysis of the synthesized compounds was performed. Antimicrobial activity was determined by the agar diffusion method. Cytotoxicity was assessed based on MTT assay data.
Results and Discussion. As a result of screening for antimicrobial activity, compounds with a noticeable effect on gram-positive strains of microorganisms, particularly staphylococci that form biofilms (MIC 0.93 mM), were identified. The studied compounds had low cytotoxicity on tumor, normal, and pseudonormal cell lines.
Conclusions. The results indicate the noticeable antimicrobial activity of rhodanine derivatives with an indole fragment in the molecules, which indicates the prospects for an in-depth study of this class of compounds.
References
Lesyk RB, Zimenkovsky BS. 4-Thiazolidones: centenarian history, current status and perspectives for modern organic and medicinal chemistry. Current Organic Chemistry. 2004;8(16):1547-77. DOI:10.2174/1385272043369773 DOI: https://doi.org/10.2174/1385272043369773
Tomašić T, Peterlin Mašič L. Rhodanine as a scaffold in drug discovery: a critical review of its biological activities and mechanisms of target modulation. Expert opinion on drug discovery. 2012;7(7):549-60. DOI:10.1517/17460441.2012.688743 DOI: https://doi.org/10.1517/17460441.2012.688743
Kumari A, Singh RK. Medicinal chemistry of indole derivatives: Current to future therapeutic prospectives. Bioorganic chemistry. 2019;89:103021. DOI:10.1016/j.bioorg.2019.103021 DOI: https://doi.org/10.1016/j.bioorg.2019.103021
Balouiri M, Sadiki M, Ibnsouda SK. Methods for in vitro evaluating antimicrobial activity: A review. Journal of pharmaceutical analysis. 2016;6(2):71-9. DOI:10.1016/j.jpha.2015.11.005 DOI: https://doi.org/10.1016/j.jpha.2015.11.005
Konechnyi Y, Lozynskyi A, Ivasechko I, Dumych T, Paryzhak S, Hrushka O, Partyka U, Pasichnyuk I, Khylyuk D, Lesyk R. 3-[5-(1H-Indol-3-ylmethylene)-4-oxo-2-thioxothiazolidin-3-yl]-propionic Acid as a Potential Polypharmacological Agent. Scientia Pharmaceutica. 2023;91(1):13. DOI:10.3390/scipharm91010013 DOI: https://doi.org/10.3390/scipharm91010013
Konechnyi YT, Lozynskyi AV, Horishny VY, Konechna RT, Vynnytska RB, Korniychuk OP, Lesyk RB. Synthesis of indoline-thiazolidinone hybrids with antibacterial and antifungal activities. Biopolymers and Cell. 2020;36(5):381-91. DOI:10.7124/bc.000A3A DOI: https://doi.org/10.7124/bc.000A3A
Holota S, Kryshchyshyn A, Derkach H, Trufin Y, Demchuk I, Gzella A, Grellier P, Lesyk R. Synthesis of 5-enamine-4-thiazolidinone derivatives with trypanocidal and anticancer activity. Bioorganic chemistry. 2019;86:126-36. DOI:10.1016/j.bioorg.2019.01.045 DOI: https://doi.org/10.1016/j.bioorg.2019.01.045
Downloads
Published
How to Cite
Issue
Section
License
Copyright (c) 2024 Pharmaceutical Review / Farmacevtičnij časopis

This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
The authors who publish their materials in this journal agree with the following terms:
- Authors reserve the right to authorship of their work and assign to the journal the right to first publish this work under the terms of the Creative Commons Attribution License, which allows other persons to freely distribute the published work with a mandatory reference to the authors of original work and the first publication of work in this journal
.
- Authors have the right to make independent extra-exclusive work agreements in the form they are published by this journal (for example, posting work in an electronic repository of an institution or publishing as part of a monograph), provided that the link to the first publication of the work in this journal is maintained.
Journal policy allows and encourages publication of manuscripts on the Internet (for example, in institutions repositories or on personal websites), both before the publication of this manuscript and during its editorial review, as it contributes to productive scientific discussion and positively affects the efficiency and dynamics of the citation of the published work (see The Effect of Open Access).