Highly potent macrocyclic BACE-1 inhibitors incorporating a hydroxyethylamine core: Design, synthesis and X-ray crystal structures of enzyme inhibitor complexes
A series of P1-P3 linked macrocyclic BACE-1 inhibitors containing a hydroxyethylamine (HEA) isostere scaffold has been synthesized. All inhibitors comprise a toluene or N-phenylmethanesulfonamide P2 moiety. Excellent BACE-1 potencies, both in enzymatic an
Sandgren, Veronica,Agback, Tatiana,Johansson, Per-Ola,Lindberg, Jimmy,Kvarnstr?m, Ingemar,Samuelsson, Bertil,Belda, Oscar,Dahlgren, Anders
p. 4377 - 4389
(2012/08/28)
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