Synthesis and antibacterial study of unsaturated Mannich ketones

Tamás Lóránd, Béla Kocsis, Pál Sohár, Gergely Nagy, Gyula Kispál, Hans Georg Krane, Horst Schmitt, Edgar Weckert

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27 Citations (Scopus)

Abstract

Several Mannich ketones of 2-arylmethylenecycloalkanones were synthesised using the classical acid-catalysed Mannich reaction. Antibacterial activity of these new water-soluble compounds was reported against Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus, Staphylococcus saprophyticus, Micrococcus luteus and Bacillus subtilis standard strains. Human cell line cytotoxicity of our new compounds was evaluated against HeLa cell lines. Some compounds showed low cytotoxicity (41.52 nM mL-1 for 14 and 46.60 nM mL-1 for 18) and proved to be efficient antibacterial agents against the Gram-positive strains. Minimum inhibitory concentrations varied from 1.56 to 100 μg mL-1. The mechanism of action was examined, too.

Original languageEnglish
Pages (from-to)705-717
Number of pages13
JournalEuropean Journal of Medicinal Chemistry
Volume36
Issue number9
DOIs
Publication statusPublished - Sep 1 2001

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Keywords

  • Antibacterial activity
  • Cytotoxicity
  • Mannich ketone
  • NMR

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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