Identification of Thiazolidinones Spiro-Fused to Indolin-2-ones as Potent and Selective Inhibitors of the Mycobacterium tuberculosis Protein Tyrosine Phosphatase B

被引：290

作者：

Vintonyak, Viktor V. ^{[1
]}

Warburg, Karin ^{[1
,2
]}

Kruse, Holger ^{[4
]}

Grimme, Stefan ^{[4
]}

Huebel, Katja ^{[1
]}

Rauh, Daniel ^{[3
]}

Waldmann, Herbert ^{[1
,2
]}

机构：

[1] Max Planck Inst Mol Physiol, Abt Chem Biol, D-44227 Dortmund, Germany

[2] Tech Univ Dortmund, Fachbereich Chem Biol, Fak Chem, D-44227 Dortmund, Germany

[3] Max Planck Gesell, Chem Genom Ctr, Dortmund, Germany

[4] Univ Munster, Inst Organ Chem, D-4400 Munster, Germany

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2010年 / 49卷 / 34期

关键词：

chemical biology; circular dichroism; enzyme inhibitors; phosphatases; tuberculosis; ELECTRONIC CIRCULAR-DICHROISM; BIOLOGY-ORIENTED SYNTHESIS; DENSITY-FUNCTIONAL THEORY; OPTICAL-ROTATORY DISPERSION; NATURAL-PRODUCTS; ABSOLUTE-CONFIGURATIONS; SPECTRA; ROTATION; MPTPB; DISCOVERY;

D O I：

10.1002/anie.201002138

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

(Figure Presented) The best of 40000: Detailed structureactivity- relationship studies revealed key structural elements of indolin-2-on-3- spirothiazolidinones (see example) and their appropriate configuration for strong inhibitory activity against the pathophysiologically relevant title protein. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

引用

页码：5902 / 5905

页数：4

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