Identification of small-molecule inhibitors of the Abeta-ABAD interaction

  • Bioorg Med Chem Lett. 2006 Sep 1;16(17):4657-60. doi: 10.1016/j.bmcl.2006.05.099.
Yuli Xie  1 ,  Shixian Deng ,  Zhenzhang Chen ,  Shidu Yan ,  Donald W Landry
Affiliations
  • 1. Department of Medicine, Columbia University, New York, NY 10032, USA.
PMID: 16781151 DOI: 10.1016/j.bmcl.2006.05.099
Abstract

The interaction of amyloid beta peptide (Abeta) and Abeta-binding alcohol dehydrogenase (ABAD) was recently implicated in the pathogenesis of Alzheimer's disease (AD). Using an ELISA-based screening assay, we identified frentizole, an FDA-approved immunosuppressive drug, as a novel inhibitor of the Abeta-ABAD interaction. Analysis of the frentizole structure-activity relationship led to identification of a novel benzothiazole urea with a 30-fold improvement in potency.

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