Synthetic chalcones as efficient inhibitors of Mycobacterium tuberculosis protein tyrosine phosphatase PtpA

被引：93

作者：

Chiaradia, Louise Domeneghini ^{[2
]}

Mascarello, Alessandra ^{[2
]}

Purificacao, Marcela ^{[1
]}

Vernal, Javier ^{[1
]}

Sechini Cordeiro, Marlon Norberto ^{[2
]}

Zenteno, Maria Emilia ^{[1
]}

Villarino, Andrea ^{[1
]}

Nunes, Ricardo Jose ^{[2
]}

Yunes, Rosendo Augusto ^{[2
]}

Terenzi, Hernan ^{[1
]}

机构：

[1] Univ Fed Santa Catarina, Dept Bioquim, Ctr Ciencias Biol, BR-88040900 Florianopolis, SC, Brazil

[2] Univ Fed Santa Catarina, Dept Quim, BR-88040900 Florianopolis, SC, Brazil

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 23期

关键词：

Chalcones; Tuberculosis; PtpA;

D O I：

10.1016/j.bmcl.2008.09.105

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In the search for lead compounds for new drugs for tuberculosis, the activity of 38 synthetic chalcones were assayed for their potential inhibitory action towards a protein tyrosine phosphatase from Mycobacterium tuberculosis - PtpA. The compounds were obtained by aldolic condensation between aldehydes and acetophenones, under basic conditions. Five compounds presented moderate or good activity. The structure - activity analysis reveals that the predominant factor for the activity is the molecule planarity/hydrophobicity and the nature of the substituents. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：6227 / 6230

页数：4

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