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

Eur J Med Chem. 2009 May;44(5):1823-9. doi: 10.1016/j.ejmech.2008.10.038. Epub 2008 Nov 7.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Alcohols / chemistry
  • Amino Alcohols / pharmacology
  • Antifungal Agents / chemistry*
  • Antifungal Agents / pharmacology*
  • Candida albicans
  • Chitin / biosynthesis
  • Chitin Synthase / drug effects
  • Ergosterol / biosynthesis
  • Hyphae / drug effects
  • Ketones / chemistry
  • Ketones / pharmacology
  • Protein Biosynthesis / drug effects
  • Quantitative Structure-Activity Relationship*

Substances

  • Amino Alcohols
  • Antifungal Agents
  • Ketones
  • Chitin
  • Chitin Synthase
  • Ergosterol