Preliminary evaluation of thiazolidinone- and pyrazoline-related heterocyclic derivatives as potential antimalarial agents

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 differen...

Full description

Saved in:
Bibliographic Details
Published in:Biopolimery i kletka 2020-02, Vol.36 (1), p.47-59
Main Authors: Kryshchyshyn-Dylevych, A. P., Zelisko, N. I., Grellier, P., Lesyk, R. B.
Format: Article
Language:English
Subjects:
Antimalarial agents
Antiprotozoal agents
Chemical Sciences
Erythrocytes
Life Sciences
Microbiology and Parasitology
Plasmodium falciparum
Structure-activity relationships
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:0233-7657
1993-6842
DOI:10.7124/bc.000A20