53385-82-3Relevant academic research and scientific papers
Structural, spectral and thermal studies of substituted N-(2-pyridyl)-N′-phenylthioureas
Valdés-Martínez, Jesús,Hernández-Ortega, Simón,Espinosa-Pérez, Georgina,Presto, Carmina A,Hermetet, Anne K,Haslow, Kristin D,Ackerman, Lily J,Szczepura, Lisa F,Goldberg, Karen I,Kaminsky, Werner,West, Douglas X
, p. 77 - 87 (2002)
N-2-(3-picolyl)-N′-phenylthiourea, 3PicTuPh, monoclinic, P21/n, a = 7.617(2) b = 7.197(5), c = 22.889(5) ?, β = 94.63(4)°, V = 1250.7(1) ?3 and Z = 4; N-2-(4-picolyl)-N′-phenylthiourea, 4PicTuPh, triclinic, P-1, a = 7.3960(5), b = 7.
2-aminothiazoles as therapeutic leads for prion diseases
Gallardo-Godoy, Alejandra,Gever, Joel,Fife, Kimberly L.,Silber, B. Michael,Prusiner, Stanley B.,Renslo, Adam R.
experimental part, p. 1010 - 1021 (2011/04/25)
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 relationships (SAR) and the identification of lead compounds that are orally absorbed and achieve high brain concentrations in animals. The new aminothiazole analogue (5-methylpyridin-2-yl)-[4-(3-phenylisoxazol-5-yl)-thiazol-2-yl]-amine (27), for example, exhibited an EC50 of 0.94 μM in prion-infected neuroblastoma cells (ScN2a-cl3) and reached a concentration of ~25 μM in the brains of mice following three days of oral administration in a rodent liquid diet. The studies described herein suggest 2-aminothiazoles as promising new leads in the search for effective therapeutics for prion diseases.
