Design, synthesis, and in vivo characterization of a novel series of tetralin amino imidazoles as γ-secretase inhibitors: Discovery of PF-3084014 was written by Brodney, Michael A.;Auperin, David D.;Becker, Stacey L.;Bronk, Brian S.;Brown, Tracy M.;Coffman, Karen J.;Finley, James E.;Hicks, Carol D.;Karmilowicz, Michael J.;Lanz, Thomas A.;Liston, Dane;Liu, Xingrong;Martin, Barbara-Anne;Nelson, Robert B.;Nolan, Charles E.;Oborski, Christine E.;Parker, Christine P.;Richter, Karl E. G.;Pozdnyakov, Nikolay;Sahagan, Barbara G.;Schachter, Joel B.;Sokolowski, Sharon A.;Tate, Barbara;Wood, Douglas E.;Wood, Kathleen M.;Van Deusen, Jeffrey W.;Zhang, Lei. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2011.Safety of Methyl 2-methyl-2-(4-nitro-1H-imidazol-1-yl)propanoate The following contents are mentioned in the article:
A novel series of tetralin containing amino imidazoles, derived from modification of the corresponding Ph acetic acid derivatives is described. Replacement of the amide led to identification of a potent series of tetralin-amino imidazoles with robust central efficacy. The reduction of brain Aβ in guinea pigs in the absence of changes in B-cells suggested a potential therapeutic index with respect to APP processing compared with biomarkers of notch related toxicity. Optimization of the FTOC to plasma concentrations at the brain Aβ EC50 lead to the identification of compound I (PF-3084014) which was selected for clin. development. This study involved multiple reactions and reactants, such as Methyl 2-methyl-2-(4-nitro-1H-imidazol-1-yl)propanoate (cas: 865774-07-8Safety of Methyl 2-methyl-2-(4-nitro-1H-imidazol-1-yl)propanoate).
Methyl 2-methyl-2-(4-nitro-1H-imidazol-1-yl)propanoate (cas: 865774-07-8) belongs to imidazole derivatives. The solubility of imidazoles in ethers is lower than that in alcohols and decreases with increasing chain length of the ethers . In contrast, the solubility of benzimidazoles in alcohols (C3–C6) is higher than in water and generally decreases with a Imidazole derivatives have antibacterial, antifungal and anticancer functionality. It interacts with DNA and also binds to protein and stops cell division.Safety of Methyl 2-methyl-2-(4-nitro-1H-imidazol-1-yl)propanoate
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem