Matos, Maria João Correia Pinto Carvalho deSantana Penín, María LourdesJaneiro, PatriciaQuezada González, Elías NeftalíUriarte Villares, EugenioGonzález Díaz, HumbertoViña Castelao, María DoloresOrallo Cambeiro, Francisco2021-08-182021-08-182008Matos, 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-12-012393-906980-20-0http://hdl.handle.net/10347/26848The 12th 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 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 isoformeng© 2008 The author(s). Published by MDPI, Basel, Switzerland. Open Accessbook part10.3390/ecsoc-12-01239open access