Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and Efficacious g-Secretase Inhibitors

Discovery of a series of pyrazolopiperidine sulfonamide based g-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...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010-04, Vol.20 (7), p.2195-2199
Main Authors: Ye, Xiaocong M, Konradi, Andrei W, Smith, Jenifer, Xu, Ying-Zi, Dressen, Darren, Garofalo, Albert W, Marugg, Jennifer, Sham, Hing L, Truong, Anh P, Jagodzinski, Jacek, Pleiss, Michael, Zhang, Hongbin, Goldbach, Erich, Sauer, John-Michael, Brigham, Elizabeth, Bova, Michael, Basi, Guriqbal S
Format: Article
Language:English
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Summary:Discovery of a series of pyrazolopiperidine sulfonamide based g-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. AB:
ISSN:0960-894X
DOI:10.1016/j.bmcl.2010.02.039