基于分子建模的取代哌啶类γ-分泌酶抑制剂的设计、合成及活性研究
Molecular-modeling based design, synthesis, and activity of substituted piperidines as gamma-secretase inhibitors.
作者信息
Gundersen Eric, Fan Kristi, Haas Kimberly, Huryn Donna, Steven Jacobsen J, Kreft Anthony, Martone Robert, Mayer Scott, Sonnenberg-Reines June, Sun Shaiu-Ching, Zhou Hua
机构信息
Chemical and Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543-8000, USA.
出版信息
Bioorg Med Chem Lett. 2005 Apr 1;15(7):1891-4. doi: 10.1016/j.bmcl.2005.02.006.
Alzheimer's disease (AD) is a debilitating disease widely thought to be associated with the accumulation of beta amyloid (Abeta) in the brain. Inhibition of gamma-secretase, one of the enzymes responsible for Abeta production, may be a useful strategy for the treatment of AD. Described below is a series of gamma-secretase inhibitors designed from a scaffold identified by a ROCS [J. Comput. Chem.1996, 17, 1653] search of the corporate database.
阿尔茨海默病（AD）是一种使人衰弱的疾病，普遍认为与大脑中β淀粉样蛋白（Aβ）的积累有关。γ-分泌酶是负责产生Aβ的酶之一，抑制γ-分泌酶可能是治疗AD的一种有效策略。以下介绍了一系列基于通过ROCS[《计算机化学杂志》1996年，第17卷，第1653页]在公司数据库搜索中确定的一个支架设计的γ-分泌酶抑制剂。
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