Structure guided P1' modifications of HEA derived β-secretase inhibitors for the treatment of Alzheimer's disease.
作者： Holger Monenschein , Daniel B. Horne , Michael D. Bartberger , Stephen A. Hitchcock , Thomas T. Nguyen
DOI: 10.1016/J.BMCL.2012.04.060
关键词:
摘要: The synthesis and SAR of a series BACE-1 hydroxyethyl amine inhibitors containing substitutions on spirocyclobutyl moiety is described. Selectivity against cathepsin D, related aspartyl protease with potential off target toxicity, improved microsomal stability exemplified.
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