Article

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

Department of Medicine, Columbia University, New York, NY 10032, USA.
Bioorganic & Medicinal Chemistry Letters (Impact Factor: 2.33). 10/2006; 16(17):4657-60. DOI: 10.1016/j.bmcl.2006.05.099
Source: PubMed

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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