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
Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici (Dip. 63), Università di Roma La Sapienza, Piazzale A. Moro 5, I-00185 Roma, Italy.
J Med Chem. 2005 Jun 30;48(13):4220-3. doi: 10.1021/jm050172c.
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.
合成了吡咯乙胺类化合物1 - 12、18 - 23以及相关的氨基醇类化合物13 - 15、24 - 27，并对其进行了单胺氧化酶A和B（MAO - A和MAO - B）的测试。总体而言，发现氨基酮类化合物1 - 12、18 - 23是强效且选择性的MAO - A抑制剂。特别地，化合物18对MAO - A同工酶的抑制作用比参考药物更强且更具选择性。有趣的是，氨基醇25选择性地抑制MAO - B酶，可能是设计更强效和选择性MAO - B抑制剂的先导化合物。
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