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Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63. Epub 2006 Feb 10.

Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors.

Author information

1
Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. lorin.thompson@bms.com

Abstract

The synthesis, evaluation, and structure-activity relationships of a series of succinoyl lactam inhibitors of the Alzheimer's disease gamma-secretase are described. Beginning with a screening hit with broad proteinase activity, optimization provided compounds with both high selectivity for inhibition of gamma-secretase and high potency in cellular assays of A beta reduction. The SAR and early in vivo properties of this series of inhibitors will be presented.

PMID:
16473009
DOI:
10.1016/j.bmcl.2006.01.055
[Indexed for MEDLINE]

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