Synthesis, molecular modeling studies, and selective inhibitory activity against monoamine oxidase of N,N′-bis[2-oxo-2H-benzopyran]-3-carboxamides

被引：32

作者：

Chimenti, Franco

Secci, Daniela

Bolasco, Adriana

Chimenti, Paola

Granese, Arianna

Carradori, Simone

Befani, Olivia

Turini, Paola

Alcaro, Stefano

Ortuso, Francesco

机构：

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

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

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

[4] Univ Catanzaro, Dipartimento Sci Farm Biol Complesso Nini Barbier, I-88021 Catanzaro, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 15期

关键词：

monoamine oxidase; reversible monoamine oxidase-A inhibitors; selective monoamine oxidase-A inhibitors (1H)-benzopyran-derivatives;

D O I：

10.1016/j.bmcl.2006.04.026

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

A novel series of N,N'-bis[2-oxo-2H-1-benzopyran]-3-carboxamide derivatives have been synthesized and investigated for the ability to inhibit the activity of the A and B isoforms of monoamine oxidase (MAO). Some of the synthesized compounds show good selective inhibitory activity against the MAO-A isoform. Both the MAO-A and -B isoforms, deposited in the Protein Data Bank as the 2BXR and 1GOS models, respectively, were considered in a computational study performed with docking techniques on the most active and selective inhibitors. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：4135 / 4140

页数：6

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