753029-44-6Relevant academic research and scientific papers
KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine
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
, p. 1527 - 1531 (2004)
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 (IC50=3.4 nM) was designed and synthesized.
