|
|||||
|
|
KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine |
|
| Authors: | Kimura Tooru Shuto Daisuke Kasai Soko Liu Ping Hidaka Koushi Hamada Takashi Hayashi Yoshio Hattori Chinatsu Asai Masashi Kitazume Shinobu Saido Takaomi C Ishiura Shoichi Kiso Yoshiaki |
| Institution: | Department of Medicinal Chemistry, Center for Frontier Research in Medicinal Science, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8412, Japan. |
| Abstract: | Recently, we reported a novel substrate-based octapeptide BACE1 inhibitor KMI-008 containing hydroxymethylcarbonyl (HMC) isostere as a transition-state mimic. Using KMI-008 as a lead compound, a small-sized and highly potent BACE1 inhibitor KMI-370 (IC(50)=3.4 nM) was designed and synthesized. |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ | |