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

被引:26
作者
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
机构
[1] Univ Roma La Sapienza, Dipartimento Studi Farmaceut, Ist Pasteur, Fdn Cenci Bolognetti, I-00185 Rome, Italy
[2] Univ Roma La Sapienza, Dipartimento Sci Biochim, I-00185 Rome, Italy
[3] Univ Roma La Sapienza, CNR, Ist Biol & Patol Mol, I-00185 Rome, Italy
[4] Ist Super Sanita, Dipartimento Farmaco, I-00161 Rome, Italy
关键词
D O I
10.1021/jm050172c
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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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收藏
页码:4220 / 4223
页数:4
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