Antifungal unsaturated cyclic Mannich ketones and amino alcohols: Study of mechanism of action

Béla Kocsis, Ildikó Kustos, Ferenc Kilár, Adrien Nyul, Péter B. Jakus, Szilárd Kerekes, Victor Villarreal, Laszlo Prokai, Tamás Lóránd

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Abstract

The antifungal activity of some known unsaturated Mannich ketones and their amino alcohols has been reported and the mechanism of antifungal action has been studied. The inhibition of the fungal ergosterol, chitin, protein synthesis and pseudohypha formation was investigated. According to our results, Mannich ketones can influence the development of pseudohyphae of Candida albicans strains. In addition, they are able to induce significant changes in the protein composition of this fungal strain. Some of our Mannich ketones have shown inhibitory effect on the fungal chitin synthase enzyme. QSAR studies were also carried out.

Original languageEnglish
Pages (from-to)1823-1829
Number of pages7
JournalEuropean Journal of Medicinal Chemistry
Volume44
Issue number5
DOIs
Publication statusPublished - 1 May 2009

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Keywords

  • Antifungal activity
  • Chitin synthase
  • Mannich ketone
  • Protein synthesis
  • Pseudohypha
  • QSAR

Cite this

Kocsis, B., Kustos, I., Kilár, F., Nyul, A., Jakus, P. B., Kerekes, S., ... Lóránd, T. (2009). Antifungal unsaturated cyclic Mannich ketones and amino alcohols: Study of mechanism of action. European Journal of Medicinal Chemistry, 44(5), 1823-1829. https://doi.org/10.1016/j.ejmech.2008.10.038