Discovery of sulfonamide–pyrazole γ-secretase inhibitors

Matthew N. Mattson,Martin L. Neitzel,David A. Quincy,Christopher M. Semko,Albert W. Garofalo,Pamela S. Keim,Andrei W. Konradi,Michael A. Pleiss,Hing L. Sham,Elizabeth F. Brigham,Erich G. Goldbach,Hongbin Zhang,John-Michael Sauer,Guriqbal S. Basi

Bioorganic & Medicinal Chemistry Letters（2010）

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摘要

Utilizing a pharmacophore hypothesis, previously described γ-secretase inhibiting HTS hits were evolved into novel tricyclic sulfonamide–pyrazoles, with high in vitro potency, good brain penetration, low metabolic stability, and high clearance.

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关键词

Alzheimer’s disease,γ-secretase inhibitor,Sulfonamide

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