Design, synthesis, and biological activities of pyrrolylethanoneamine derivatives, a novel class of monoamine oxidases inhibitors.

Article Details

Citation

Copy to clipboard

Di Santo R, Costi R, Roux A, Artico M, Befani O, Meninno T, Agostinelli E, Palmegiani P, Turini P, Cirilli R, Ferretti R, Gallinella B, La Torre F

Design, synthesis, and biological activities of pyrrolylethanoneamine derivatives, a novel class of monoamine oxidases inhibitors.

J Med Chem. 2005 Jun 30;48(13):4220-3.

PubMed ID

15974574 [ View in PubMed

]

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Moclobemide	Amine oxidase [flavin-containing] B	Ki (nM)	100000	N/A	N/A	Details
Selegiline	Amine oxidase [flavin-containing] B	Ki (nM)	970	N/A	N/A	Details