| Literature DB >> 22098494 |
Zhong-Yue Sun1, Theodros Asberom, Thomas Bara, Chad Bennett, Duane Burnett, Inhou Chu, John Clader, Mary Cohen-Williams, David Cole, Michael Czarniecki, James Durkin, Gioconda Gallo, William Greenlee, Hubert Josien, Xianhai Huang, Lynn Hyde, Nicholas Jones, Irina Kazakevich, Hongmei Li, Xiaoxiang Liu, Julie Lee, Malcolm Maccoss, Mihir B Mandal, Troy McCracken, Amin Nomeir, Robert Mazzola, Anandan Palani, Eric M Parker, Dmitri A Pissarnitski, Jun Qin, Lixin Song, Giuseppe Terracina, Monica Vicarel, Johannes Voigt, Ruo Xu, Lili Zhang, Qi Zhang, Zhiqiang Zhao, Xiaohong Zhu, Zhaoning Zhu.
Abstract
Cyclic hydroxyamidines were designed and validated as isosteric replacements of the amide functionality. Compounds with these structural motifs were found to be metabolically stable and to possess highly desirable pharmacokinetic profiles. These designs were applied in the identification of γ-secretase modulators leading to highly efficacious agents for reduction of central nervous system Aβ(42) in various animal models.Entities:
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Year: 2011 PMID： 22098494 DOI： 10.1021/jm201407j
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446