具有治疗阿尔茨海默病潜力的氨基己内酰胺 γ-分泌酶抑制剂。
Amino-caprolactam γ-secretase inhibitors showing potential for the treatment of Alzheimer's disease.
机构信息
Department of Medicinal Chemistry, Elan Pharmaceuticals, South San Francisco, CA 94080, United States.
出版信息
Bioorg Med Chem Lett. 2011 Jun 15;21(12):3715-20. doi: 10.1016/j.bmcl.2011.04.079. Epub 2011 May 1.
Herein we describe the structure-activity relationship (SAR) of amino-caprolactam analogs derived from amino-caprolactam benzene sulfonamide 1, highlighting affects on the potency of γ-secretase inhibition, selectivity for the inhibition of APP versus Notch processing by γ-secretase and selected pharmakokinetic properties. Amino-caprolactams that are efficacious in reducing the cortical Aβ(x-40) levels in FVB mice via a single 100 mpk IP dose are highlighted.
在此，我们描述了氨基己内酰胺苯磺酰胺 1 的类似物的结构-活性关系 (SAR)，重点介绍了对 γ-分泌酶抑制活性、对 γ-分泌酶抑制 APP 与 Notch 加工的选择性以及所选药代动力学性质的影响。通过单次 100mpk IP 剂量，能够有效降低 FVB 小鼠皮质 Aβ(x-40)水平的氨基己内酰胺类化合物被突出强调。
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