Bioorganic and Medicinal Chemistry Letters p. 1 - 6 (1999)
Update date:2022-08-05
Topics:
Oza, Vibha B.
Petrassi, H. Michael
Purkey, Hans E.
Kelly, Jeffery W.
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.
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