Design, synthesis, and biological activities of pyrrolylethanoneamine derivatives, a novel class of monoamine oxidases inhibitors |
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| Authors: | Di Santo Roberto Costi Roberta Roux Alessandra Artico Marino Befani Olivia Meninno Tiziana Agostinelli Enzo Palmegiani Paola Turini Paola Cirilli Roberto Ferretti Rosella Gallinella Bruno La Torre Francesco |
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| Affiliation: | Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici (Dip. 63), Università di Roma La Sapienza, Piazzale A. Moro 5, I-00185 Roma, Italy. roberto.disanto@uniroma1.it |
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| Abstract: | Pyrrolylethanoneamines 1-12, 18-23 and related amino alcohols 13-15, 24-27 were synthesized and tested against monoamine oxidases A and B (MAO-A and MAO-B) enzymes. In general, aminoketones 1-12, 18-23 were found to be potent and selective MAO-A inhibitors. In particular, 18 was more potent and selective against the MAO-A isoenzyme than reference drugs. Interestingly, amino alcohol 25 selectively inhibited MAO-B enzyme and could be a lead compound for designing more potent and selective MAO-B inhibitors. |
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