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

Xiaocong M Ye,Andrei W Konradi,Jenifer Smith,Ying-Zi Xu,Darren Dressen,Albert W Garofalo,Jennifer Marugg,Hing L Sham,Anh P Truong,Jacek Jagodzinski,Michael Pleiss,Hongbin Zhang,Erich Goldbach,John-Michael Sauer,Elizabeth Brigham,Michael Bova,Guriqbal S Basi

Bioorganic & medicinal chemistry letters（2010）

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摘要

Discovery of a series of pyrazolopiperidine sulfonamide based gamma-secretase inhibitors and its SAR evolution is described. Significant increases in APP potency on the pyrazolopiperidine scaffold over the original N-bicyclic sulfonamide scaffold were achieved and this potency increase translated in an improved in vivo efficacy.

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