- Design, synthesis, and biological activities of pyrrolylethanoneamine derivatives, a novel class of monoamine oxidases inhibitors.
Design, synthesis, and biological activities of pyrrolylethanoneamine derivatives, a novel class of monoamine oxidases inhibitors.
Journal of medicinal chemistry (2005-06-25)
Roberto Di Santo, Roberta Costi, Alessandra Roux, Marino Artico, Olivia Befani, Tiziana Meninno, Enzo Agostinelli, Paola Palmegiani, Paola Turini, Roberto Cirilli, Rosella Ferretti, Bruno Gallinella, Francesco La Torre
PMID15974574
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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