Published in
American Chemical Society, Journal of Medicinal Chemistry, 13(48), p. 4220-4223, 2005
DOI: 10.1021/jm050172c
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Design, Synthesis, and Biological Activities of Pyrrolylethanoneamine Derivatives, a Novel Class of Monoamine Oxidases Inhibitors
,
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
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- Must not violate ACS ethical Guidelines
- Must obtain written permission from Editor
- Must not violate ACS ethical Guidelines
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.