Synthesis of new chalcone derivatives bearing 2,4-thiazolidinedione and benzoic acid moieties as potential anti-bacterial agents

A series of chalcone derivatives bearing the 2,4-thiazolidinedione and benzoic acid moieties (8a–s) were synthesized, characterized, and evaluated for their anti-bacterial activity. Among the tested compounds, the most effective were 8a, 8h, 8k, 8n and 8q with MIC value in the range of 0.5–4 μg/mL against six Gram-positive bacteria (including multidrug-resistant clinical isolates). None of the compounds exhibited any activity against the Gram-negative bacteria Escherichia coli 1356 and E. coli 1682 at 64 μg/mL.

Graphical abstractA series of new chalcone derivatives bearing 2,4-thiazolidinedione and benzoic acid moieties were synthesized, characterized, and evaluated for their anti-bacterial activity.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► New hybrid compounds possessing chalcone and 2,4-thiazolidinedione were synthesized. ► Some compounds exhibited more potent than control medicines against MRSA and QRSA. ► 8a showed strongest activity against MRSA 3506 with the MIC value of 0.5 μg/mL.