Biopolym. Cell. 2020; 36(1):48-60.
http://dx.doi.org/10.7124/bc.000A20
Bioorganic Chemistry
Preliminary evaluation of thiazolidinone- and pyrazoline-related heterocyclic derivatives as potential antimalarial agents
1Kryshchyshyn-Dylevych A. P., 1Zelisko N. I., 2Grellier P., 1Lesyk R. B.
  1. Danylo Halytsky Lviv National Medical University
    69, Pekarska Str., Lviv, Ukraine, 79010
  2. National Museum of Natural History, UMR 7245 CNRS MCAM, Sorbonne Universités
    CP 52, 57 Rue Cuvier, Paris 75005, France

Abstract

Aim. Synthesis of a series of thiazolidinone- and pyrazoline-related compounds. In vitro screening of antiplasmodial activity of versatile heterocyclic derivatives. Methods: organic wet synthesis, analytical and spectral methods, pharmacological screening, SAR analysis. Results. A series of different thiazolidinone- and pyrazoline-based derivatives was screened against Plasmodium falciparum in in vitro assays. 5-(Z)-Arylidene-2-arylidenehydrazono-3-(4-hydroxyphenyl)-4-thiazolidinones showed high growth inhibition rates with the IC50–2.32-2.39 µM. 5-Bromo-1-[2-[3-(4-chlorophenyl)-5-(4-methoxyphenyl)-3,4-dihydropyrazol-2-yl]-2-oxoethyl]indoline-2,3-dione 3 was the most active compound among tested with the IC50–1.81 µM. Based on the screening data some structure-activity relationships were derived. Conclusions. A set of different thiazolidinone- and pyrazoline-related derivatives with antitrypanosomal and anticancer properties was screened against Plasmodium falciparum. Hit-compounds inhibiting growth of the parasite at micromolar concentrations were identified. The obtained results provide further avenues to develop more potent antimalarial agents on the base of investigated classes of small drug-like molecules.
Keywords: thiazolidinone, pyrazoline, antimalarial activity, SAR analysis
Full text: (PDF, in English)

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