Synthesis and evaluation of inhibitors of transthyretin amyloid formation based on the non-steroidal anti-inflammatory drug, flufenamic acid

PW Baures, VB Oza, SA Peterson, JW Kelly

Index: Baures, Paul W.; Oza, Vibha B.; Peterson, Scott A.; Kelly, Jeffery W. Bioorganic and Medicinal Chemistry, 1999 , vol. 7, # 7 p. 1339 - 1347

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Citation Number: 126

Abstract

A light scattering-based amyloid fibril formation assay was employed to evaluate potential inhibitors of transthyretin (TTR) amyloid fibril formation in vitro. Twenty nine aromatic small molecules, some with homology to flufenamic acid (a known non-steroidal anti-inflammatory drug) were tested to identify important structural features for inhibitor efficacy. The results of these experiments and earlier data suggest that likely inhibitors will have aromatic-based ...