Bioorganic & Medicinal Chemistry Letters 2003-03-24

Inhibitors of Abeta production: solid-phase synthesis and SAR of alpha-hydroxycarbonyl derivatives.

Owen B Wallace, David W Smith, Milind S Deshpande, Craig Polson, Kevin M Felsenstein

文献索引：Bioorg. Med. Chem. Lett. 13(6) , 1203-6, (2003)

全文：HTML全文

摘要

Inhibitors of amyloid-beta (Abeta) protein production have been widely pursued as a potential treatment for Alzheimer's disease. Following the identification of a 5 microM screening hit, SAR was initiated using solid-phase synthetic techniques. Two series of alpha-hydroxy esters and ketones which are sub-micromolar inhibitors of Abeta production were identified. The most potent alpha-hydroxyketone identified is approximately 30-fold more potent than the initial lead.