Abstract
Ten oxazoles bearing a C(4) carboxyl group were synthesized and evaluated as transthyretin (TTR) amyloid fibril inhibitors. Substituting aryls at the C(2) position of the oxazole ring reveals that a 3,5-dichlorophenyl substituent significantly reduced amyloidogenesis. The efficacy of these inhibitors was enhanced further by installing an ethyl, a propyl, or a CF3 group at the C(5) position. The CF3 substitution at C(5) also improves the TTR binding selectivity over all the other proteins in human blood. © 2004 Elsevier Ltd. All rights reserved.
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Razavi, H., Powers, E. T., Purkey, H. E., Adamski-Werner, S. L., Chiang, K. P., Dendle, M. T. A., & Kelly, J. W. (2005). Design, synthesis, and evaluation of oxazole transthyretin amyloidogenesis inhibitors. Bioorganic and Medicinal Chemistry Letters, 15(4), 1075–1078. https://doi.org/10.1016/j.bmcl.2004.12.022
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