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https://doi.org/10.5562/cca2890

Comparison of Inhibitory Activities of meta and para Substituted N-aryl 3-Hydroxypyridin-4-one Mannosides Towards Type 1 Fimbriated E. coli

Vesna Petrović Peroković ; University of Zagreb, Faculty of Science, Department of Chemistry, Horvatovac 102a, HR-10000 Zagreb, Croatia
Rosana Ribić ; University of Zagreb, Faculty of Science, Department of Chemistry, Horvatovac 102a, HR-10000 Zagreb, Croatia
Željka Car ; University of Zagreb, Faculty of Science, Department of Chemistry, Horvatovac 102a, HR-10000 Zagreb, Croatia
Srđanka Tomić ; University of Zagreb, Faculty of Science, Department of Chemistry, Horvatovac 102a, HR-10000 Zagreb, Croatia

Puni tekst: engleski, pdf (649 KB) str. 237-242 preuzimanja: 350* citiraj
APA 6th Edition
Petrović Peroković, V., Ribić, R., Car, Ž. i Tomić, S. (2016). Comparison of Inhibitory Activities of meta and para Substituted N-aryl 3-Hydroxypyridin-4-one Mannosides Towards Type 1 Fimbriated E. coli. Croatica Chemica Acta, 89 (2), 237-242. https://doi.org/10.5562/cca2890
MLA 8th Edition
Petrović Peroković, Vesna, et al. "Comparison of Inhibitory Activities of meta and para Substituted N-aryl 3-Hydroxypyridin-4-one Mannosides Towards Type 1 Fimbriated E. coli." Croatica Chemica Acta, vol. 89, br. 2, 2016, str. 237-242. https://doi.org/10.5562/cca2890. Citirano 16.11.2019.
Chicago 17th Edition
Petrović Peroković, Vesna, Rosana Ribić, Željka Car i Srđanka Tomić. "Comparison of Inhibitory Activities of meta and para Substituted N-aryl 3-Hydroxypyridin-4-one Mannosides Towards Type 1 Fimbriated E. coli." Croatica Chemica Acta 89, br. 2 (2016): 237-242. https://doi.org/10.5562/cca2890
Harvard
Petrović Peroković, V., et al. (2016). 'Comparison of Inhibitory Activities of meta and para Substituted N-aryl 3-Hydroxypyridin-4-one Mannosides Towards Type 1 Fimbriated E. coli', Croatica Chemica Acta, 89(2), str. 237-242. https://doi.org/10.5562/cca2890
Vancouver
Petrović Peroković V, Ribić R, Car Ž, Tomić S. Comparison of Inhibitory Activities of meta and para Substituted N-aryl 3-Hydroxypyridin-4-one Mannosides Towards Type 1 Fimbriated E. coli. Croatica Chemica Acta [Internet]. 2016 [pristupljeno 16.11.2019.];89(2):237-242. https://doi.org/10.5562/cca2890
IEEE
V. Petrović Peroković, R. Ribić, Ž. Car i S. Tomić, "Comparison of Inhibitory Activities of meta and para Substituted N-aryl 3-Hydroxypyridin-4-one Mannosides Towards Type 1 Fimbriated E. coli", Croatica Chemica Acta, vol.89, br. 2, str. 237-242, 2016. [Online]. https://doi.org/10.5562/cca2890

Sažetak
In uropathogenic Escherichia coli, mannose-specific adhesion is mediated by the FimH adhesin located at the tip of type 1 fimbriae. Novel mannosylated N-aryl substituted 3-hydroxypyridin-4ones with meta substituents on the aryl part of the molecule were prepared, and their inhibitory properties towards the adhesion of E. coli to guinea pig erythrocytes explored using the hemagglutination assay. These results were compared with inhibitory potencies of analogous para derivatives. The assays revealed greater preference of FimH towards para substituted compounds in general, with p-nitro and p-methoxy substituted substrates being much more effective then the hydrophobic p-methyl compound. When substituents are in meta position the positive affect on the binding of compounds in the FimH binding site was observed with all compounds tested but the structure with an alkyl group was shown to be the most effective one. This study provides guidelines for the rational design of novel, more effective series of FimH antagonists.

Creative Commons License This work is licensed under a Creative Commons Attribution 4.0 International License.

Ključne riječi
N-aryl 3-hydroxypyridin-4-one mannosides; FimH antagonist; hemagglutination; E. coli

Hrčak ID: 167415

URI
https://hrcak.srce.hr/167415

Posjeta: 489 *