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Bioorg Med Chem Lett. 2007 Oct 1;17(19):5330-5. Epub 2007 Aug 15.

Small conformationally restricted piperidine N-arylsulfonamides as orally active gamma-secretase inhibitors.

Author information

1
Department of Chemical Research, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07302, USA. hubert.josien@spcorp.com

Abstract

The design and development of a new class of small 2,6-disubstituted piperidine N-arylsulfonamide gamma-secretase inhibitors is reported. Lowering molecular weight including the use of conformational constraint led to compounds with less CYP 3A4 liability compared to early leads. Compounds active orally in lowering Abeta levels in Tg CRND8 mice were identified as potential treatments for Alzheimer's disease.

PMID:
17761417
DOI:
10.1016/j.bmcl.2007.08.013
[Indexed for MEDLINE]

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