Peer-reviewed veterinary case report
Fluorinated piperidine acetic acids as gamma-secretase modulators.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2010
- Authors:
- Stanton, Matthew G et al.
- Affiliation:
- Department of Drug Design and Optimization · United States
- Species:
- rodent
Abstract
We report herein a novel series of difluoropiperidine acetic acids as modulators of gamma-secretase. Synthesis of 2-aryl-3,3-difluoropiperidine analogs was facilitated by a unique and selective beta-difluorination with Selectfluor. Compounds 1f and 2c were selected for in vivo assessment and demonstrated selective lowering of Abeta42 in a genetically engineered mouse model of APP processing. Moreover, in a 7-day safety study, rats treated orally with compound 1f (250mg/kg per day, AUC(0-24)=2100microMh) did not exhibit Notch-related effects.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/20005099/