Structure-activity relationship and docking studies of thiazolidinedione-type compounds with monoamine oxidase B

被引：22

作者：

Carroll, Richard T. ^{[1
,2
]}

Dluzen, Dean E. ^{[1
,2
,3
,4
]}

Stinnett, Hilary ^{[1
,2
]}

Awale, Prabha S. ^{[1
,2
]}

Funk, Max O. ^{[5
]}

Geldenhuys, Werner J. ^{[1
,2
]}

机构：

[1] Northeastern Ohio Univ Coll Med & Pharm, Coll Med, Dept Pharmaceut Sci, Rootstown, OH 44272 USA

[2] Northeastern Ohio Univ Coll Med & Pharm, Coll Pharm, Dept Pharmaceut Sci, Rootstown, OH 44272 USA

[3] Northeastern Ohio Univ Coll Med & Pharm, Coll Med, Dept Anat & Neurobiol, Rootstown, OH 44272 USA

[4] Northeastern Ohio Univ Coll Med & Pharm, Coll Pharm, Dept Anat & Neurobiol, Rootstown, OH 44272 USA

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 16期

关键词：

Enzyme; Amplex-Red; Kynuramine; Pharmacophore; MPTP; GAMMA AGONIST PIOGLITAZONE; MOUSE MODEL; PARKINSONS-DISEASE; INHIBITORS;

D O I：

10.1016/j.bmcl.2011.06.060

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The neuroprotective activity of pioglitazone and rosiglitazone in the MPTP parkinsonian mouse prompted us to evaluate a set of thiazolidinedione (TZD) type compounds for monoamine oxidase A and B inhibition activity. These compounds were able to inhibit MAO-B over several log units of magnitude (82 nM to 600 mu M). Initial structure-activity relationship studies identified key areas to modify the aromatic substituted TZD compounds. Primarily, substitutions on the aromatic group and the TZD nitrogen were key areas where activity was enhanced within this group of compounds. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：4798 / 4803

页数：6

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