- Phe*-Ala-based pentapeptide mimetics are BACE inhibitors: P2 and P3 SAR.
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We describe herein the syntheses and evaluation of a series of C-termini pyridyl containing Phe*-Ala-based BACE inhibitors (5-19). In conjunction with four fixed residues at the P1 (Phe), P1' (Ala), P2' (Val), and P2' cap (Pyr.), rather detailed SAR modifications at P2 and P3 positions were pursued. The promising inhibitors emerging from this SAR investigation, 12 and 17 demonstrated very good enzyme potency (IC(50)=45 nM) and cellular activity (IC(50)=0.4 microM).
- Lamar, Jason,Hu, Jingdan,Bueno, Ana Belen,Yang, Hsiu-Chiung,Guo, Deqi,Copp, James D,McGee, James,Gitter, Bruce,Timm, David,May, Patrick,McCarthy, James,Chen, Shu-Hui
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p. 239 - 243
(2007/10/03)
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- Synthesis of enantiomerically pure D- and L-armentomycin and its difluoro analogues from aspartic acid
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The synthesis of both enantiomers of 2-amino-4,4-dichlorobutanoic acid (armentomycin) and their fluoro analogues from aspartic acid via 2-amino-4-oxobutanoic acid protected with hexafluoroacetone is described.
- Winkler, Dirk,Burger, Klaus
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p. 1419 - 1421
(2007/10/03)
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