2-Aminothiazoles as therapeutic leads for prion diseases

A Gallardo-Godoy, J Gever, KL Fife…

Index: Gallardo-Godoy, Alejandra; Gever, Joel; Fife, Kimberly L.; Silber, B. Michael; Prusiner, Stanley B.; Renslo, Adam R. Journal of Medicinal Chemistry, 2011 , vol. 54, # 4 p. 1010 - 1021

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Citation Number: 74

Abstract

2-Aminothiazoles are a new class of small molecules with antiprion activity in prion-infected neuroblastoma cell lines (J. Virol. 2010, 84, 3408). We report here structure− activity studies undertaken to improve the potency and physiochemical properties of 2-aminothiazoles, with a particular emphasis on achieving and sustaining high drug concentrations in the brain. The results of this effort include the generation of informative structure− activity ...