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2005
Oxazole derivatives
R 0220
Design, Synthesis, and Evaluation of Oxazole Transthyretin Amyloidogenesis
— In order to identify novel transthyretin (TTR) inhibitors with enhanced
25- 125 Inhibitors.
potency and improved binding selectivity to TTR over other plasma proteins, oxazoles
containing a carboxylic acid, an alkyl group and a halogenated aromatic pharmacophore are synthesized. Oxazoles (VII) are obtained in low to moderate overall yields
via a diazo transfer reaction cf. (I)→(II), the in situ formed thioimidate (V) from a phosphazene intermediate, and reaction of (V) with acyl chlorides or anhydrides, followed
by hydrolysis. Several compounds inhibit TTR amyloidogenesis in vitro and two bind
TTR in human plasma with modest selectivity. In particular, (VIIa) and (VIIc) completely inhibit fibril formation and bind to TTR in the presence of other plasma proteins.
— (RAZAVI, H.; POWERS, E. T.; PURKEY, H. E.; ADAMSKI-WERNER, S. L.;
CHIANG, K. P.; DENDLE, M. T. A.; KELLY*, J. W.; Bioorg. Med. Chem. Lett. 15
(2005) 4, 1075-1078; Dep. Chem., Scripps Res. Inst., San Diego, La Jolla, CA 92037,
USA; Eng.) — H. Hoennerscheid
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