Shaw Duncan, Best Jonathan, Dinnell Kevin, Nadin Alan, Shearman Mark, Pattison Christine, Peachey James, Reilly Michael, Williams Brian, Wrigley Jonathan, Harrison Timothy
Department of Medicinal Chemistry, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK.
Bioorg Med Chem Lett. 2006 Jun 1;16(11):3073-7. doi: 10.1016/j.bmcl.2005.12.083. Epub 2006 Apr 17.
The 3,4-fused sulfamides, sulfonamides and sulfone have been identified as highly potent gamma-secretase inhibitors. Evaluation of the SAR of substitution within these series has allowed the identification of a range of compounds which significantly reduce brain A beta in transgenic mouse models and thus have potential as possible treatments for Alzheimer's disease.
3,4-稠合的磺酰胺、磺胺和砜已被鉴定为高效的γ-分泌酶抑制剂。对这些系列中取代基的构效关系进行评估，已鉴定出一系列化合物，这些化合物在转基因小鼠模型中能显著降低脑内β-淀粉样蛋白，因此具有作为阿尔茨海默病可能治疗方法的潜力。
