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Acta Pharmaceutica, Vol.55 No.4 December 2005. -

Antibacterial and antifungal activity of N-phthaloylamino acid hydroxamates 1-3 -C6H4CO2N-x-CONHOH, x = amino acid residues of glycine, ß-alanine and D-phenylglycine- was examined against 44 strains of Gram-positive and Gram-negative bacteria, and 10 species of yeasts. The level of antimicrobial effects was established using the in vitro agar assay and the standard broth dilution susceptibility test. N-phthaloyl-D-phenylglycine-hydroxamic acid 3, the substance with the highest lipophilicity log P, showed the best antibacterial activity, especially against Gram-negative bacteria. Minimum inhibitory concentration of 3 was 0.008 mg mL-1 in the activity against Yersinia enterocolitica O3, confirmed by a large inhibition zone 30 mm by the diffusion test. Hydroxamates inhibit growth by chelation of PDF enzyme metal in both Gram-positive and Gram-negative bacteria, and LpxC enzyme in Gram-negative enzyme. Phthalimides apear to contribute to inhibition by destabilizing m-RNA. Antifungal activity of substances 1-3 is not very expressed.

hydroxamic acid; phthalimide; antibacterial activity; lipophilicity



Autor: JULIJA MATIJEVIĆ-SOSA - ZDENKA CVETNIĆ -

Fuente: http://hrcak.srce.hr/



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