Synthesis and evaluation of anthranilic acid-based transthyretin amyloid fibril inhibitors

VB Oza, HM Petrassi, HE Purkey, JW Kelly

文献索引：Oza, Vibha B.; Petrassi, H. Michael; Purkey, Hans E.; Kelly, Jeffery W. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 1 p. 1 - 6

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被引用次数: 73

摘要

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 ...