RT Journal Article
T1 Curcumin–Coumarin Hybrid Analogues as Multitarget Agents in Neurodegenerative Disorders
A1 Quezada González, Elías Neftalí
A1 Rodríguez Enríquez, Fernanda
A1 Laguna Francia, María de los Reyes
A1 Cutrín Gómez, Elena
A1 Otero Espinar, Francisco Javier
A1 Uriarte Villares, Eugenio
A1 Viña Castelao, María Dolores
K1 Curcumin
K1 Curcumin–coumarin hybrids
K1 Neuroprotection
K1 Monoamine oxidase inhibition
K1 Cholinesterase inhibition
K1 Scavenging activity
AB Neurodegenerative diseases have a complex nature which highlights the need for multitarget ligands to address the complementary pathways involved in these diseases. Over the last decade, many innovative curcumin-based compounds have been designed and synthesized, searching for new derivatives having anti-amyloidogenic, inhibitory of tau formation, as well as anti-neuroinflammation, antioxidative, and AChE inhibitory activities. Regarding our experience studying 3-substituted coumarins with interesting properties for neurodegenerative diseases, our aim was to synthesize a new series of curcumin–coumarin hybrid analogues and evaluate their activity. Most of the 3-(7-phenyl-3,5-dioxohepta-1,6-dien-1-yl)coumarin derivatives 11–18 resulted in moderated inhibitors of hMAO isoforms and AChE and BuChE activity. Some of them are also capable of scavenger the free radical DPPH. Furthermore, compounds 14 and 16 showed neuroprotective activity against H2O2 in SH-SY5Y cell line. Nanoparticles formulation of these derivatives improved this property increasing the neuroprotective activity to the nanomolar range. Results suggest that by modulating the substitution pattern on both coumarin moiety and phenyl ring, ChE and MAO-targeted derivatives or derivatives with activity in cell-based phenotypic assays can be obtained
PB MDPI
YR 2021
FD 2021
LK http://hdl.handle.net/10347/26788
UL http://hdl.handle.net/10347/26788
LA eng
NO Molecules 2021, 26(15), 4550; https://doi.org/Molecules 2021, 26(15), 4550; https://doi.org/10.3390/molecules26154550
NO This research was funded by Consellería de Cultura, Educación e Ordenación Universitaria (EM2014/016) and Centro Singular de Investigación de Galicia and the European Regional De-velopment Fund (ERDF) (accreditation 2016–2019, ED431G/05)
DS Minerva
RD 24 abr 2026