氨基甲酸酯连接的N-烷基磺酰胺作为γ-分泌酶抑制剂
Carbamate-appended N-alkylsulfonamides as inhibitors of gamma-secretase.
作者信息
Bergstrom Carl P, Sloan Charles P, Lau Wai-Yu, Smith David W, Zheng Ming, Hansel Steven B, Polson Craig T, Corsa Jason A, Barten Donna M, Felsenstein Kevin M, Roberts Susan B
机构信息
Department of Discovery Chemistry, Research and Development, Bristol-Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA.
出版信息
Bioorg Med Chem Lett. 2008 Jan 15;18(2):464-8. doi: 10.1016/j.bmcl.2007.11.102. Epub 2007 Dec 3.
The synthesis and gamma-secretase inhibition data for a series of carbamate-appended N-alkylsulfonamides are described. Carbamate 54 was found to significantly reduce brain Abeta in transgenic mice. 54 was also found to possess markedly improved brain levels in transgenic mice compared to previously disclosed 1 and 2.
描述了一系列氨基甲酸酯连接的N-烷基磺酰胺的合成及γ-分泌酶抑制数据。发现氨基甲酸酯54能显著降低转基因小鼠脑中的β-淀粉样蛋白（Aβ）。与先前公开的化合物1和2相比，还发现54在转基因小鼠中的脑内水平有显著提高。
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