合成查耳酮作为结核分枝杆菌蛋白酪氨酸磷酸酶PtpA的有效抑制剂。
Synthetic chalcones as efficient inhibitors of Mycobacterium tuberculosis protein tyrosine phosphatase PtpA.
作者信息
Chiaradia Louise Domeneghini, Mascarello Alessandra, Purificação Marcela, Vernal Javier, Cordeiro Marlon Norberto Sechini, Zenteno María Emilia, Villarino Andréa, Nunes Ricardo José, Yunes Rosendo Augusto, Terenzi Hernán
机构信息
Departamento de Química, Universidade Federal de Santa Catarina, Campus Trindade, 88040-900 Florianópolis, SC, Brazil.
出版信息
Bioorg Med Chem Lett. 2008 Dec 1;18(23):6227-30. doi: 10.1016/j.bmcl.2008.09.105. Epub 2008 Oct 5.
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.
在寻找抗结核新药先导化合物的过程中，对38种合成查尔酮针对结核分枝杆菌蛋白酪氨酸磷酸酶PtpA的潜在抑制活性进行了测定。这些化合物是在碱性条件下通过醛与苯乙酮之间的羟醛缩合反应获得的。有5种化合物表现出中等或良好的活性。构效关系分析表明，活性的主要影响因素是分子的平面性/疏水性以及取代基的性质。
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