Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors (Part II).

Xiaocong M Ye,Andrei W Konradi,Jenifer Smith,Danielle L Aubele,Albert W Garofalo,Jennifer Marugg, Marty L Neitzel,Chris M Semko,Hing L Sham,Minghua Sun,Anh P Truong,Jing Wu,Hongbin Zhang,Erich Goldbach,John-Michael Sauer,Elizabeth F Brigham,Michael Bova,Guriqbal S Basi

Bioorganic & medicinal chemistry letters（2010）

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摘要

Significant improvement in metabolic stability on the pyrazolopiperidine scaffold over the original series were achieved and this stability improvement translated in an improved in vivo efficacy.

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