- Design and synthesis of potent hydroxyethylamine (HEA) BACE-1 inhibitors carrying prime side 4,5,6,7-tetrahydrobenzazole and 4,5,6,7- tetrahydropyridinoazole templates
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A set of low molecular weight compounds containing a hydroxyethylamine (HEA) core structure with different prime side alkyl substituted 4,5,6,7-tetrahydrobenzazoles and one 4,5,6,7-tetrahydropyridinoazole was synthesized. Striking differences were observed on potencies in the BACE-1 enzymatic and cellular assays depending on the nature of the heteroatoms in the bicyclic ring, from the low active compound 4 to inhibitor 6, displaying BACE-1 IC50 values of 44 nM (enzyme assay) and 65 nM (cell-based assay).
- Sund, Christian,Belda, Oscar,Borkakoti, Neera,Lindberg, Jimmy,Derbyshire, Dean,Vrang, Lotta,Hamelink, Elizabeth,Hgren, Cathrine,Woestenenk, Esmeralda,Wikstroem, Kristina,Eneroth, Anders,Lindstroem, Erik,Kalayanov, Genadiy
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p. 6721 - 6727,7
(2012/12/12)
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- Process for the production of cyclopropanenitrile derivatives
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A process for the production of cyclopropanenitrile derivatives. A diol of the formula: STR1 wherein R1 and R2 are the same or different and each is a hydrogen atom, a C1 -C6 alkyl group, branched or unbranched,
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