Synthesis and evaluation of anthranilic acid-based transthyretin amyloid fibril inhibitors
Synthesis and evaluation of anthranilic acid-based transthyretin amyloid fibril inhibitors
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DOI：
10.1016/s0960-894x(98)00696-9
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发表时间：
1999-01-04
影响因子：
2.7
通讯作者：
Kelly, JW
中科院分区：
文献类型：
--
作者：
Oza, VB;Petrassi, HM;Kelly, JW
合成了8个小分子化合物，用于评价N-取代邻氨基苯甲酸类化合物的构效关系。这些分子是通过邻氨基苯甲酸甲酯的苄基化或芳基化反应合成的。使用基于光散射的淀粉样蛋白原纤维形成测定来评估体外转甲状腺素蛋白（TTR）淀粉样蛋白原纤维形成的潜在抑制剂。间羧基苯基化和邻三氟甲基苯基化邻氨基苯甲酸是有效的抑制剂，将对其进行进一步的SAR和结构分析，（C）1998 Elsevier Science Ltd.保留所有权利。
Eight small molecules were synthesized to evaluate the structure activity relationships (SAR) of N-substituted anthranilic acids. The molecules were synthesized by benzylation or arylation of methyl anthranilate. A light scattering-based amyloid fibril formation assay was used to evaluate potential inhibitors of transthyretin (TTR) amyloid fibril formation in vitro. The m-carboxyphenylated and o-trifluoromethylphenylated anthranilic acids are potent inhibitors that will be subjected to further SAR and structural analysis, (C) 1998 Elsevier Science Ltd. All rights reserved.