RT Book,_Section
T1 Design, Synthesis and Pharmacological Evaluation of New Coumarin Derivatives as Monoamine Oxidase A and B Inhibitors
A1 Matos, Maria João Correia Pinto Carvalho de
A1 Santana Penín, María Lourdes
A1 Janeiro, Patricia
A1 Quezada González, Elías Neftalí
A1 Uriarte Villares, Eugenio
A1 González Díaz, Humberto
A1 Viña Castelao, María Dolores
A1 Orallo Cambeiro, Francisco
AB With the aim to find out the structural features for the MAO inhibitory activity and selectivity, in the present communication we report the design, synthesis and pharmacological evaluation of a new series of coumarin derivatives with 4-methyl or cycloalkene or benzene ring condensed in the 3,4 position. The substituents in this new scaffold were introduced in the 5, 7 and/or 8 positions of the coumarin moiety. The synthesized compounds 1-13 were evaluated as MAO A and B inhibitors using clorgyline and selegiline, respectively, as reference inhibitors, showing, most of them, activities in the nanomolar range. Compounds 6 (IC50 = 1.18 nM) and 10 (IC50 = 1.48 nM), show higher activity than selegiline (IC50 = 19.60 nM), and high MAO-B selectivity with 100-fold and 1600-fold inhibition levels, with respect to the MAO-A isoform
PB MDPI
SN 3-906980-20-0
YR 2008
FD 2008
LK http://hdl.handle.net/10347/26848
UL http://hdl.handle.net/10347/26848
LA eng
NO Matos, M.J.; Santana, L.; Janeiro, P.; Quezada, E.; Uriarte, E.; González-Díaz, H.; Viña, D.; Orallo, F. Design, Synthesis and Pharmacological Evaluation of New Coumarin Derivatives as Monoamine Oxidase A and B Inhibitors, in Proceedings of the 12th International Electronic Conference on Synthetic Organic Chemistry, 1–30 November 2008, MDPI: Basel, Switzerland, doi:10.3390/ecsoc-12-01239
NO The 12th International Electronic Conference on Synthetic Organic Chemistry session Bioorganic Chemistry and Natural Products
NO We are grateful to the Xunta de Galicia (INCITE07PXI203030ES, PGIDIT05BTF20302PR and INCITE08PXIB203022PR) and Ministerio de Sanidad y Consumo (FIS PI061537 and PI061457) for financial support.
DS Minerva
RD 24 abr 2026