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

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 48卷 / 13期

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.

引用

页码：4220 / 4223

页数：4

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