Design, synthesis, and structure–activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline γ-secretase inhibitors

Anh P. Truong,Danielle L. Aubele,Gary D. Probst,Martin L. Neitzel,Chris M. Semko,Simeon Bowers,Darren B. Dressen,Roy K. Hom,Andrei W. Konradi,Hing L. Sham,Albert W. Garofalo,Pamela S. Keim,Jing Wu,Michael S. Dappen,Karina Wong,Erich Goldbach,Kevin P. Quinn,John-Michael Sauer,Elizabeth F. Brigham,William Wallace,Lan Nguyen,Susanna S. Hemphill,Michael P. Bova,Guriqbal S. Basi

Design, synthesis, and structure–activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline γ-secretase inhibitors

2009

Abstract In this Letter, we report our strategy to design potent and metabolically stable γ-secretase inhibitors that are efficacious in reducing the cortical Aβx-40 levels in FVB mice via a single PO dose.

Keywords:

Oral administration
Organic chemistry
Amyloid precursor protein secretase
Pyrazole
In vivo
Amyloid precursor protein
Chemical synthesis
Stereochemistry
Structure–activity relationship
Enzyme inhibitor
Chemistry
Enzyme

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