99802-75-2Relevant academic research and scientific papers
Aminothiazoles as γ-secretase modulators
Lübbers, Thomas,Flohr, Alexander,Jolidon, Synese,Jacobsen, Helmut,Ozmen, Laurence,Baumann, Karlheinz,David-Pierson, Pascale
, p. 6554 - 6558 (2011)
We herein report the discovery of a new γ-secretase modulator class with an aminothiazole core starting from a HTS hit (3). Synthesis and SAR of this series are discussed. These novel compounds demonstrate moderate to good in vitro potency in inhibiting amyloid beta (Aβ) peptide production. Overall c-secretase is not inhibited but the formation of the aggregating, toxic Aβ42 peptide is shifted to smaller non-aggregating Ab peptides. Compound 15 reduced brain Abβ42 in vivo in APPSwe transgenic mice at 30 mg/kg p.o.
PREPARATION OF PYRIMIDINES AND PYRIDINES FROM ALKYL KETONES AND NITRILES IN PRESENCE OF PHOSPHORYL CHLORIDE
Zielinski, Wojciech
, p. 1639 - 1644 (2007/10/02)
The reaction of alkyl ketones with nitriles in the presence of POCl3 has been examined.It has been found that N-vinylimidoyl dichlorophosphates initially formed react further with excess nitriles or ketones to afford pyrimidine or pyridine derivatives, respectively.
