| Literature DB >> 21742495 |
Zehong Wan1, Adrian Hall, Yingxia Sang, Jia-Ning Xiang, Eric Yang, Beverley Smith, David C Harrison, Guang Yang, Haihua Yu, Helen S Price, Jian Wang, Julie Hawkins, Lit-Fui Lau, Matthew R Johnson, Tina Li, Wei Zhao, William L Mitchell, Xiaobo Su, Xiaomin Zhang, Yanjiao Zhou, Yun Jin, Zhaolong Tong, Ziqiang Cheng, Ishrut Hussain, John D Elliott, Yasuji Matsuoka.
Abstract
SAR of a novel series of pyridine-derived γ-secretase modulators is described. Compound 5 was found to be a potent modulator in vitro, which on further profiling, was found to decrease Aβ42 and Aβ40, and maintain (or increase) the levels of total Aβ. Furthermore, representative compounds 1 and 5 demonstrated in vivo efficacy to lower Aβ42 in the brain without altering Notch processing in the peripheral.Entities:
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Year: 2011 PMID： 21742495 DOI： 10.1016/j.bmcl.2011.06.042
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823