In 2011,Gallardo-Godoy, Alejandra; Gever, Joel; Fife, Kimberly L.; Silber, B. Michael; Prusiner, Stanley B.; Renslo, Adam R. published 《2-Aminothiazoles as Therapeutic Leads for Prion Diseases》.Journal of Medicinal Chemistry published the findings.Computed Properties of C4H7NO2S The information in the text is summarized as follows:
2-Aminothiazoles are a new class of small mols. with antiprion activity in prion-infected neuroblastoma cell lines. We report here structure-activity studies undertaken to improve the potency and physiochem. 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 analog (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. In the experimental materials used by the author, we found Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Computed Properties of C4H7NO2S)
Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Halogenation, in which one or more hydrogen atoms of an amine is replaced by a halogen atom, occurs with chlorine, bromine, and iodine, as well as with some other reagents, notably hypochlorous acid (HClO). With primary amines the reaction proceeds in two stages, producing N-chloro- and N,N-dichloro-amines, RNHCl and RNCl2, respectively. With tertiary amines, an alkyl group may be displaced by a halogen.Computed Properties of C4H7NO2S
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