Piperidine-derived Gamma-secretase Modulators

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 2010 Jan 9

PMID 20056541

Citations 12

Authors

Adrian Hall

Richard L Elliott

Gerard M P Giblin

Ishrut Hussain

James Musgrave

Alan Naylor

Rosemary Sasse

Beverley Smith

Affiliations

Soon will be listed here.

Abstract

This Letter details the SAR of a novel series of piperidine-derived gamma-secretase modulators. Compound 10h was found to be a potent modulator in vitro, which on further profiling, was found to decrease Abeta42, increase Abeta38 and have no effect on Abeta40 levels. Furthermore, 10h demonstrated excellent pharmacokinetic parameters in the mouse, rat and dog in addition to good CNS penetration in the mouse.

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