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Design, Spectroscopy, and Assessment of Cholinesterase Inhibition and Antimicrobial Activities of Novel Coumarin–Thiadiazole Hybrids

  • Dariusz Karcz
  • , Karolina Starzak
  • , Ewa Ciszkowicz
  • , Katarzyna Lecka-Szlachta
  • , Daniel Kamiński
  • , Bernadette Creaven
  • , Anna Miłoś
  • , Hollie Jenkins
  • , Lidia Ślusarczyk
  • , Arkadiusz Matwijczuk

Research output: Contribution to journalArticlepeer-review

Abstract

A novel series of coumarin–thiadiazole hybrids, derived from substituted coumarin-3-carboxylic acids was isolated and fully characterized with the use of a number of spectroscopic techniques and XRD crystallography. Several of the novel compounds showed intensive fluorescence in the visible region, comparable to that of known coumarin-based fluorescence standards. Moreover, the new compounds were tested as potential antineurodegenerative agents via their abil-ity to act as acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitors. Compared to the commercial standards, only a few compounds demonstrated moderate AChE and BuChE activities. Moreover, the novel derivatives were tested for their antimicrobial activity against a panel of pathogenic bacterial and fungal species. Their lack of activity and toxicity across a broad range of biochemical assays, together with the exceptional emission of some hybrid molecules, highlights the possible use of a number of the novel hybrids as potential fluorescence standards or fluorescence imaging agents.

Original languageEnglish
Article number6314
JournalInternational Journal of Molecular Sciences
Volume23
Issue number11
DOIs
Publication statusPublished - 1 Jun 2022

Keywords

  • antimicrobial activity
  • cholinesterase inhibitors
  • coumarin
  • fluorescence imaging
  • hybrids
  • neurodegeneration
  • thiadiazole

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