TY - JOUR
T1 - Design, Spectroscopy, and Assessment of Cholinesterase Inhibition and Antimicrobial Activities of Novel Coumarin–Thiadiazole Hybrids
AU - Karcz, Dariusz
AU - Starzak, Karolina
AU - Ciszkowicz, Ewa
AU - Lecka-Szlachta, Katarzyna
AU - Kamiński, Daniel
AU - Creaven, Bernadette
AU - Miłoś, Anna
AU - Jenkins, Hollie
AU - Ślusarczyk, Lidia
AU - Matwijczuk, Arkadiusz
N1 - Publisher Copyright:
© 2022 by the authors. Li-censee MDPI, Basel, Switzerland.
PY - 2022/6/1
Y1 - 2022/6/1
N2 - 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.
AB - 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.
KW - antimicrobial activity
KW - cholinesterase inhibitors
KW - coumarin
KW - fluorescence imaging
KW - hybrids
KW - neurodegeneration
KW - thiadiazole
UR - http://www.scopus.com/inward/record.url?scp=85131262111&partnerID=8YFLogxK
U2 - 10.3390/ijms23116314
DO - 10.3390/ijms23116314
M3 - Article
C2 - 35682998
AN - SCOPUS:85131262111
SN - 1661-6596
VL - 23
JO - International Journal of Molecular Sciences
JF - International Journal of Molecular Sciences
IS - 11
M1 - 6314
ER -