The activities of some 4-morpholino-5-nitro- and 4,5-dinitro-imidazole derivatives with respect to several Candida species were evaluated. It is established that 4,5-dinitroimidazole derivatives constitute an important group of compounds possessing antifungal activity against Candida species. Some analogs showed moderate antifungal ability in vitro, especially in relation well-known antifungals such as flucytosine (5FC). The best results of antifungal action were obtained for 1-(3-bromo-2-hydroxypropyl)-2-methyl-4,5-dinitroimidazole (3c), 1-(3-bromo-2-oxopropyl)-2-methyl-4,5-dinitroimidazole (4c) and 2-methyl-1-phenacyl-4,5-dinitroimidazole (2b). The latter compound proved to be effective against Candida sake S-1 (in contrast to inactive 5FC).
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References
J. H. Meurman, E. Siikala, M. Richardson, et al., in: Communicating Current Research and Educational Topics and Trends in Applied Microbiology, Microbiology Book Series, A. Méndez-Vilas (ed.), Badajoz, Formatex 1 (2007), pp. 719 – 731.
L. De Luca, Curr. Med. Chem., 13, 1 – 23 (2006).
E. R. Dabbs, S. Naidoo, C. Lephoto, et al, Antimicrob. Agents Chemother., 47, 1476 – 1478 (2003).
D. Olender, J. Żwawiak, V. Lukianchuk, et al., Eur. J. Med. Chem., 44, 645 – 652 (2009).
A. Casalinuovo, P. Di Francesco, and E. Garaci, Eur. Rev. Med. Pharmacol. Sci., 8, 69 – 77 (2004).
L. Zaprutko, U. Wrzeciono, M. Gajdziñski, et al., Pharmazie, 47, 258 – 261 (1992).
L. Zaprutko, M. Gajdziński, W. Michalska, et al., Pharmazie, 44, 817 – 820 (1989).
D. Olender, J. Żwawiak, and L. Zaprutko, J. Heterocycl. Chem., 47, 1049 – 1055 (2010).
J. Żwawiak, D. Olender, Z. Zwolska, et al., Acta Polon. Pharm.-Drug Res., 2, 229 – 233 (2008).
L. Zaprutko, D. Olender, and A. Gzella, Monatsch. Chem., 134, 1145 – 1150 (2003).
W. Bauer, W. M. M. Kirby, J. C. Sherris, et al., Am. J. Clin. Pathol., 36, 493 – 496 (1966).
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Olender, D., Zaprutko, L., Mertas, A. et al. Anti-Candida Activity of 4-Morpholino-5-Nitro- and 4,5-Dinitro-Imidazole Derivatives. Pharm Chem J 51, 1063–1067 (2018). https://doi.org/10.1007/s11094-018-1741-5
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DOI: https://doi.org/10.1007/s11094-018-1741-5