19920-87-7Relevant articles and documents
Diethylaminosulfur trifluoride-mediated intramolecular cyclization of 2-hydroxycycloalkylureas to fused bicyclic aminooxazoline compounds and evaluation of their biochemical activity against β-secretase-1 (BACE-1)
Huestis, Malcolm P.,Liu, Wendy,Volgraf, Matthew,Purkey, Hans E.,Yu, Christine,Wang, Weiru,Smith, Darin,Vigers, Guy,Dutcher, Darrin,Hunt, Kevin W.,Siu, Michael
, p. 5802 - 5807 (2013/10/01)
A series of unique bicyclic aminooxazolines were synthesized and found to exhibit micromolar inhibition of β-secretase-1 (BACE-1). The aminooxazolines were procured by an intramolecular diethylaminosulfur trifluoride (DAST)-mediated ring closure of a benz
Potent and selective cathepsin K inhibitors
Shinozuka, Tsuyoshi,Shimada, Kousei,Matsui, Satoshi,Yamane, Takahiro,Ama, Mayumi,Fukuda, Takeshi,Taki, Motohiko,Takeda, Yuko,Otsuka, Eri,Yamato, Michiko,Mochizuki, Shin-ichi,Ohhata, Keiko,Naito, Satoru
, p. 6789 - 6806 (2007/10/03)
A novel series of cathepsin K inhibitors derived from Novartis compound I is described. Optimization of the P1, P3, and P1′ units led to the identification of 4-aminophenoxyacetic acid 24b with an IC50 value of 4.8 nM, which possessed an excell