The phenolic thiazoles (V) and (VI) are synthesized from readily available N-protected α-amino amides (I) via coupling of thioamides (II) with phenacyl derivative (III) as the key step. The free amines (V) and (VI) can be transformed into their dihydrochloride salts to provide the amines as water-soluble compounds. Thiazoles (V) and (VI) are orally bioavailable and afford potent in vivo neuroprotection in models of mitochondrial toxin administration. It may be considered that these agents act as mitochondrial protecting agents. -(HARNETT*, J. J.; ROUBERT, V.; DOLO, C.; CHARNET, C.; SPINNEWYN, B.; CORNET, S.; ROLLAND, A.; MARIN, J.-G.; BIGG, D.; CHABRIER, P.-E.; Bioorg. Med. Chem. Lett. 14 (2004) 1, 157-160; Beaufour-Ipsen Res. Lab., Dep. Med. Chem., Inst. Henri Beaufour, F-91966 Les Ulis, Fr.; Eng.) -H. Hoennerscheid
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