Isothiochromenothiazoles—A Class of Fused Thiazolidinone Derivatives with Established Anticancer Activity That Inhibits Growth of Trypanosoma brucei brucei

Anna Kryshchyshyn , Danylo Kaminskyy , Igor Nektegayev , Philippe Grellier (1) , Roman Lesyk

1 MCAM - Molécules de Communication et Adaptation des Micro-organismes

Recently, thiazolidinone derivatives have been widely studied as antiparasitic agents. Previous investigations showed that fused 4-thiazolidinone derivatives (especially thiopyranothiazoles) retain pharmacological activity of their synthetic precursors-simple 5-ene-4-thiazolidinones. A series of isothiochromeno[4a,4-d][1,3] thiazoles was investigated in an in vitro assay towards bloodstream forms of Trypanosoma brucei brucei. All compounds inhibited parasite growth at concentrations in the micromolar range. The established low acute toxicity of this class of compounds along with a good trypanocidal profile indicates that isothiochromenothiazole derivatives may be promising for designing new antitrypanosomal drugs.

Mots clés: thiazolidinones; isothiochromenothiazoles; SAR analysis; Trypanosoma brucei; antitrypanosomal activity

Domaines: Microbiologie et Parasitologie; Sciences du Vivant [q-bio]; Chimie

Anna Kryshchyshyn, Danylo Kaminskyy, Igor Nektegayev, Philippe Grellier, Roman Lesyk. Isothiochromenothiazoles—A Class of Fused Thiazolidinone Derivatives with Established Anticancer Activity That Inhibits Growth of Trypanosoma brucei brucei. Scientia Pharmaceutica, 2018, 86 (4), pp.47. ⟨10.3390/scipharm86040047⟩. ⟨mnhn-02047316⟩