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Antibacterial and Antifungal Activity of Styrylquinoline Derivatives
* 1 , 2, 3 , 4 , 4 , 3 , 4 , 5
1  Division of Biologically Active Complexes and Molecular Magnets, Regional Centre of Advanced Technologies and Materials, Faculty of Science, Palacky University, Slechtitelu 27, 78371 Olomouc, Czech Republic
2  Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Comenius University, Odbojarov 10, 83232 Bratislava, Slovakia
3  Department of Infectious Diseases and Microbiology, Faculty of Veterinary Medicine, University of Veterinary and Pharmaceutical Sciences, Palackeho 1, 61242 Brno, Czech Republic
4  Institute of Chemistry, University of Silesia, 75 Pulku Piechoty 1a, 41 500 Chorzow, Poland
5  Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Comenius University, Odbojarov 10, 83232 Bratislava, Slovakia;

Published: 31 October 2018 by MDPI in 4th International Electronic Conference on Medicinal Chemistry session ECMC-4

Although the resistance is commonly known as bacterial, this problem is not related only to the domain of bacteria. The occurrence of resistant mutants of fungi is also observed. Another problem with some known antifungal drugs is that only topical applications are used due to their toxicity or limited bioavailability [1]. Thus this situation justifies the urgency to design and discover not only antibacterial but also antifungal new drugs [2].

Styrylquinoline derivatives structurally related to dichloroquinoline (e.g. chloroxine) are potential antimicrobial compounds. These derivatives were studied by Cieslik et al. [3] recently. Some of these structures expressed antifungal activity comparable with or higher than the standard fluconazole. The antibacterial effect especially against Staphylococcus strains was observed as well [3]. Based on these results, new structures were synthesized and evaluated with respect to their activity, what is presented in this work. New compounds were tested against Candida strains for their antifungal effect and against Staphylococcus and Enteroccocus strains for their antibacterial activity. Antibacterial effects were tested also against methicillin-resistant staphylococci and vancomycin-resistant enterococci.

This contribution was supported by grant FaF UK/9/2018 of the Faculty of Pharmacy of the Comenius University, grant No. UK/229/2018 of the Comenius University, NCN grant Opus:DEC-2013/09/B/NZ7/00423 of the Polish National Centre for Science and partially by SANOFI-AVENTIS Pharma Slovakia, s.r.o.

  1. Jampilek, J. Potential of agricultural fungicides for antifungal drug discovery. Expert Opin. Drug Dis. 2016, 11, 1-9.
  2. Jampilek, J. How can we bolster the antifungal drug discovery pipeline? Future Med. Chem. 2016, 8, 1393-1397.
  3. Cieslik, W.; Musiol, R.; Nycz, J.; Jampilek, J.; Vejsova, M.; Wolff, M.; Machura, B.; Polanski, J. Contribution to investigation of antimicrobial activity of styrylquinolines. Med. Chem. 2012, 20, 6960-6968.
Keywords: antibacterial activity; antifungal activity; styrylquinoline; Candida; Staphylococcus; Enterococcus