RT Book,_Section
T1 Synthesis and pharmacological evaluation of coumarins as new scaffold on the Parkinson´s disease
A1 Matos, Maria João Correia Pinto Carvalho de
A1 Viña Castelao, María Dolores
A1 Janeiro, Patricia
A1 Orallo Cambeiro, Francisco
A1 Uriarte Villares, Eugenio
A1 Santana Penín, María Lourdes
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 8-bromo-6-methyl-3-phenylcoumarin derivatives without substituent and with different number of methoxy substituent in the 3-phenyl ring. The substituent in this new scaffold was introduced in the 3', 4' and/or 5' positions of the 3-phenyl ring of the coumarin moiety. The synthesized compounds 3-6 were evaluated as MAO A and B inhibitors using R-(-)-deprenyl (selegiline) and Iproniazide as reference inhibitors, showing, most of them, MAO-B inhibitory activities in the nanomolar range. Compounds 3 (11.05±0.81 nM), 4 (3.23±0.49 nM) and 5 (7.12±0.01 nM) show higher activity than selegiline (IC50 = 19.60 nM), and high MAO-B selectivity with 9,050- fold, 30,960-fold and 14,045-fold inhibition levels, with respect to the MAO-A isoform
PB MDPI
SN 3-906980-23-5
YR 2009
FD 2009
LK http://hdl.handle.net/10347/26865
UL http://hdl.handle.net/10347/26865
LA eng
NO Santana, L.; Uriarte, E.; Orallo, F.; Janeiro, P.; Viña, D.; Matos, M. Synthesis and pharmacological evaluation of coumarins as new scaffold on the Parkinson´s disease, in Proceedings of the 13th International Electronic Conference on Synthetic Organic Chemistry, 1–30 November 2009, MDPI: Basel, Switzerland, doi:10.3390/ecsoc-13-00220
NO The 13th International Electronic Conference on Synthetic Organic Chemistry session Bioorganic Chemistry and Natural Products
NO We are grateful to the Spanish Ministerio de Sanidad y Consumo (PI061457 and PI061537) and to Xunta da Galicia (BTF20303PR, PXIB203022PR and CSA019203PR) and Fondazione Banco Sardegna (Italy) for financial support. M.J.M. also thanks MIUR for a PhD grant
DS Minerva
RD 23 abr 2026