Screening of the antiviral activity in the range of C5 and N3 substituted 4-thiazolidinone derivatives

D. V. Kaminskyy


Prospects for the search of antiviral agents among 4-thiazolidinone derivatives, as well as the optimal directions of the main core structure optimization – namely C5 and N3, have been described. As the result of the screening performed (within the Antimicrobial Acquisition and Coordinating Facility programme), the values of the antiviral activity of the target 5-substituted-4-thiazolidinones with the carboxylic group (or its derivatives) in the N3 residue on relation to a wide range of the viral panels have been determined. The active compounds, which can be regarded as promising structures in the anti-flu agent design, have been identified, as well as 3-{5-[2-chloro-3-(4-nitrophenyl)-allylidene]-4-oxo-2-thioxothiazolidine-3-yl}-propionic (1) and –succinic acids (3) have been identified has hit-compounds with a marked anti-VZV activity (SI values – 27 and 38, respectively).


4-thiazolidinones; screening; antiviral activity

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