2-Aminothiazoles as therapeutic leads for prion diseases
A Gallardo-Godoy, J Gever, KL Fife…
文献索引: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
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 ...