Matos, Maria João Correia Pinto Carvalho deViña Castelao, María DoloresJaneiro, PatriciaOrallo Cambeiro, FranciscoUriarte Villares, EugenioSantana Penín, María Lourdes2021-08-192021-08-192009Santana, 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-13-002203-906980-23-5http://hdl.handle.net/10347/26865The 13th International Electronic Conference on Synthetic Organic Chemistry session Bioorganic Chemistry and Natural ProductsWith 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 isoformeng© 2009 The author(s). Published by MDPI, Basel, Switzerland. Open Accessbook part10.3390/ecsoc-13-00220open access