环丙二胺 BACE-1 抑制剂的合成与体内评价。
Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors.
机构信息
Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA.
出版信息
Bioorg Med Chem Lett. 2011 Nov 15;21(22):6909-15. doi: 10.1016/j.bmcl.2011.06.116. Epub 2011 Jul 2.
PMID:21974952
Abstract
The synthesis, evaluation, and structure-activity relationships of a set of related constrained diaminopropane inhibitors of BACE-1 are described. The full in vivo profile of an optimized inhibitor in both normal and P-gp deficient mice is compared with data generated in normal rats.
摘要
本研究描述了一组相关的受约束二氨基丙烷 BACE-1 抑制剂的合成、评价和构效关系。在正常和 P-糖蛋白缺陷小鼠中比较了优化抑制剂的完整体内概况与在正常大鼠中产生的数据。
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