Acta Pharmaceutica, Vol. 55 No. 4, 2005.
Izvorni znanstveni članak
Antimicrobial activity of N-phthaloylamino acid hydroxamates
JULIJA MATIJEVIĆ-SOSA
ZDENKA CVETNIĆ
Sažetak
Antibacterial and antifungal activity of N-phthaloylamino acid hydroxamates 1-3 /C6H4(CO)2N-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.
Ključne riječi
hydroxamic acid; phthalimide; antibacterial activity; lipophilicity
Hrčak ID:
19044
URI
Datum izdavanja:
1.12.2005.
Posjeta: 1.967 *