4.7 Article

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

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JOURNAL OF MEDICINAL CHEMISTRY
卷 48, 期 13, 页码 4220-4223

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AMER CHEMICAL SOC
DOI: 10.1021/jm050172c

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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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