Inhibitors of Abeta production: solid-phase synthesis and SAR of alpha-hydroxycarbonyl derivatives |
| |
Authors: | Wallace Owen B Smith David W Deshpande Milind S Polson Craig Felsenstein Kevin M |
| |
Affiliation: | Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. owen.wallace@lilly.com |
| |
Abstract: | 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. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|