1336669-71-6Relevant academic research and scientific papers
Trifluoromethyl Dihydrothiazine-Based β-Secretase (BACE1) Inhibitors with Robust Central β-Amyloid Reduction and Minimal Covalent Binding Burden
Anan, Kosuke,Iso, Yasuyoshi,Oguma, Takuya,Nakahara, Kenji,Suzuki, Shinji,Yamamoto, Takahiko,Matsuoka, Eriko,Ito, Hisanori,Sakaguchi, Gaku,Ando, Shigeru,Morimoto, Kenji,Kanegawa, Naoki,Kido, Yasuto,Kawachi, Tomoyuki,Fukushima, Tamio,Teisman, Ard,Urmaliya, Vijay,Dhuyvetter, Deborah,Borghys, Herman,Austin, Nigel,Van Den Bergh, An,Verboven, Peter,Bischoff, Francois,Gijsen, Harrie J. M.,Yamano, Yoshinori,Kusakabe, Kenichi
, p. 1894 - 1910 (2019/11/22)
The β-site amyloid precursor protein cleaving enzyme 1 (BACE1, also known as β-secretase) is a promising target for the treatment of Alzheimer's disease. A pKa lowering approach over the initial leads was adopted to mitigate hERG inhibition and
β-secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease
Hilpert, Hans,Guba, Wolfgang,Woltering, Thomas J.,Wostl, Wolfgang,Pinard, Emmanuel,Mauser, Harald,Mayweg, Alexander V.,Rogers-Evans, Mark,Humm, Roland,Krummenacher, Daniela,Muser, Thorsten,Schnider, Christian,Jacobsen, Helmut,Ozmen, Laurence,Bergadano, Alessandra,Banner, David W.,Hochstrasser, Remo,Kuglstatter, Andreas,David-Pierson, Pascale,Fischer, Holger,Polara, Alessandra,Narquizian, Robert
, p. 3980 - 3995 (2013/06/27)
An extensive fluorine scan of 1,3-oxazines revealed the power of fluorine(s) to lower the pKa and thereby dramatically change the pharmacological profile of this class of BACE1 inhibitors. The CF3 substituted oxazine 89, a potent and
