Title of article
Synthesis and evaluation of succinoyl-caprolactam γ-secretase inhibitors
Author/Authors
Lorin A. Thompson، نويسنده , , Ann Y. Liauw، نويسنده , , Mercy M. Ramanjulu، نويسنده , , Padmaja Kasireddy-Polam، نويسنده , , Stephen E. Mercer، نويسنده , , Thomas P. Maduskuie، نويسنده , , Marcie Glicksman، نويسنده , , Arthur H. Roach، نويسنده , , Jere E. Meredith، نويسنده , , Ruiqin Liu، نويسنده , , Andrew P. Combs، نويسنده , , Jeffrey N. Higaki، نويسنده , , Barbara Cordell، نويسنده , , Dietmar Seiffert، نويسنده , , Robert C. Zaczek، نويسنده , , David W. Robertson، نويسنده , , Richard E. Olson، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
7
From page
2357
To page
2363
Abstract
The synthesis, evaluation, and structure–activity relationships of a series of succinoyl lactam inhibitors of the Alzheimer’s disease γ-secretase are described. Beginning with a screening hit with broad proteinase activity, optimization provided compounds with both high selectivity for inhibition of γ-secretase and high potency in cellular assays of Aβ reduction. The SAR and early in vivo properties of this series of inhibitors will be presented.
Keywords
?-Secretase inhibitors , Alzheimer’s disease , ?-Amyloid production inhibitors
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796780
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