| Literature DB >> 27560281 |
Zhiqiang Zhao1, Dmitri A Pissarnitski2, Hubert B Josien2, Thomas A Bara2, John W Clader2, Hongmei Li2, Mark D McBriar2, Murali Rajagopalan2, Ruo Xu2, Giuseppe Terracina3, Lynn Hyde3, Lixin Song3, Lili Zhang3, Eric M Parker3, Rebecca Osterman4, Alexei V Buevich4.
Abstract
The design, synthesis, SAR, and biological profile of a substituted 4-morpholine sulfonamide series of γ-secretase inhibitors (GSIs) were described. In several cases, the resulting series of GSIs reduced CYP liabilities and improved γ-secretase inhibition activity compared to our previous research series. Selected compounds demonstrated significant reduction of amyloid-β (Aβ) after acute oral dosing in a transgenic animal model of Alzheimer's disease (AD).Entities:
Keywords: Alzheimer's disease; substituted 4-morpholine sulfonamide; γ-secretase inhibitor
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Year: 2016 PMID： 27560281 DOI： 10.1016/j.ejmech.2016.08.024
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514