Pyridazine-derived γ-secretase modulators

…, Y Jin, JN Xiang, E Yang, A Eatherton, B Smith…

文献索引：Wan, Zehong; Hall, Adrian; Jin, Yun; Xiang, Jia-Ning; Yang, Eric; Eatherton, Andrew; Smith, Beverley; Yang, Guang; Yu, Haihua; Wang, Ju; Ye, Liang; Lau, Lit-Fui; Yang, Ting; Mitchell, William; Cai, Wei; Zhang, Xiaomin; Sang, Yingxia; Wang, Yonghui; Tong, Zhaolong; Cheng, Ziqiang; Hussain, Ishrut; Elliott, John D.; Matsuoka, Yasuji Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 13 p. 4016 - 4019

全文：HTML全文

被引用次数: 18

摘要

Abstract SAR of a novel series of pyridazine-derived γ-secretase modulators is described. Compound 25 was found to be a potent modulator in vitro, which on further profiling, was found to decrease Aβ42 and Aβ40, and maintain the levels of total Aβ. Furthermore, 25 demonstrated excellent pharmacokinetic parameters as well as good CNS penetration in the rat.