发现一种新型[3.2.1]苯并稠合双环磺酰胺-吡唑类化合物，作为有效、选择性的γ-分泌酶抑制剂。
Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors.
机构信息
Department of Medicinal Chemistry, Elan Pharmaceuticals, 180 Oyster Point Blvd., South San Francisco, CA 94080, USA.
出版信息
Bioorg Med Chem Lett. 2013 Feb 15;23(4):996-1000. doi: 10.1016/j.bmcl.2012.12.039. Epub 2012 Dec 21.
PMID:23312944
Abstract
Structure-activity relationship (SAR) of a novel, potent and metabolically stable series of benzo [3.2.1] bicyclic sulfonamide-pyrazoles as γ-secretase inhibitors are described. Compounds that are efficacious in reducing the cortical Aβx-40 levels in FVB mice via oral dose, as well as those with high selectivity over Notch, are highlighted.
摘要
描述了一系列新型、有效且代谢稳定的苯并[3.2.1]二环磺酰胺-吡唑类γ-分泌酶抑制剂的构效关系。通过口服剂量，这些化合物能够有效地降低 FVB 小鼠皮质 Aβx-40 水平，并且对 Notch 的选择性较高。
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