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

新型香豆素-噻二唑杂化物的设计、光谱及胆碱酯酶抑制和抗菌活性评估

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

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 ability 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.

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