Selective inhibitory activity against MAO and molecular modeling studies of 2-thiazolylhydrazone derivatives

被引：85

作者：

Chimenti, Franco

Maccioni, Elias

Secci, Daniela

Bolasco, Adriana

Chimenti, Paola

Granese, Arianna

Befani, Olivia

Turini, Paola

Alcaro, Stefano

Ortuso, Francesco

Cardia, Maria C.

Distinto, Simona

机构：

[1] Univ Roma La Sapienza, CNR, Dipartimento Studi Chim & Tecnol Sostanze Biologi, I-00185 Rome, Italy

[2] Univ Roma La Sapienza, CNR, Dipartimento Sci Biochim A Rossi Fanelli, I-00185 Rome, Italy

[3] Univ Roma La Sapienza, CNR, Ctr Biol Mol, I-00185 Rome, Italy

[4] Univ Studi Catanzaro Magna Graecia, Dipartimento Sci Farmaco Biol, I-88021 Roccelletta Di Borgia, CZ, Italy

[5] Univ Cagliari, Dipartimento Farmacochim Tecnol, I-09124 Cagliari, Italy

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2007年 / 50卷 / 04期

关键词：

D O I：

10.1021/jm060869d

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2-thiazolylhydrazone derivatives have been investigated for the ability to inhibit the activity of the A and B isoforms of monoamine oxidase (MAO) selectively. All of the compounds showed high activity against both the MAO-A and the MAO-B isoforms with pK(i) values ranging between 5.92 and 8.14 for the MAO-A and between 4.69 and 9.09 for the MAO-B isoforms. Both the MAO-A and the MAO-B isoforms, deposited in the Protein Data Bank as model 2BXR and 1GOS, respectively, were considered in a computational study performed with docking techniques on the most active and MAO-B-selective inhibitor, 18.

引用

页码：707 / 712

页数：6

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