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Synthesis of new chalcone derivatives containing a rhodanine-3-acetic acid moiety with potential anti-bacterial activity.

European journal of medicinal chemistry (2010-10-05)
Zhen-Hua Chen, Chang-Ji Zheng, Liang-Peng Sun, Hu-Ri Piao
RÉSUMÉ

With an intention to synergize the anti-bacterial activity of chalcones and rhodanine-3-acetic acid, several hybrid compounds possessing chalcone and rhodanine-3-acetic acid moieties were synthesized and tested for their anti-bacterial activity. Some compounds presented great anti-microbial activities against Gram-positive bacteria (including the multidrug-resistant clinical isolates). This class of compounds presented high potency against Staphylococcus aureus, among which the derivatives 5k with a MIC of 2 μg/mL was as active as the standard drug (norfloxacin) and less active than oxacillin. Compounds 5a-s did not inhibit the growth of Gram-negative bacteria Escherichia coli CCARM 1924 or E. coli CCARM 1356 at 64 μg/mL.

MATÉRIAUX
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Description du produit

Supelco
Norfloxacin, analytical standard, ≥98% (TLC)
Sigma-Aldrich
4-Oxo-2-thioxo-3-thiazolidinylacetic acid, ≥99%
Supelco
Norfloxacin, VETRANAL®, analytical standard