A scaffold hopping approach to identify novel monoamine oxidase B inhibitors

被引：32

作者：

Geldenhuys, Werner J. ^{[1
]}

Funk, Max O. ^{[2
]}

Van der Schyf, Cornelis J. ^{[1
]}

Carroll, Richard T. ^{[1
]}

机构：

[1] NE Ohio Med Univ, Dept Pharmaceut Sci, Rootstown, OH 44272 USA

[2] Univ Toledo, Dept Chem, Toledo, OH 43606 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 03期

关键词：

Virtual screening; Enzyme inhibition; Docking; Ligand-based; GAMMA AGONIST PIOGLITAZONE; PARKINSONS-DISEASE; IDENTIFICATION; DOCKING;

D O I：

10.1016/j.bmcl.2011.12.056

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

Monoamine oxidase B (MAO-B) inhibitors are used to treat Parkinson's disease. In this study, we searched for novel MAO-B inhibitors using a scaffold hopping approach based on our experience with the thiazolidinedione (TZD) class of compounds as MAO-B inhibitors. Several novel compounds were identified, with potencies in the low nanomolar and low micromolar range. We also found that derivatives of the natural product sulfuretin are potent MAO-A and MAO-B inhibitors. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：1380 / 1383

页数：4

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