Literature DB >> 14592525

High affinity, bioavailable 3-amino-1,4-benzodiazepine-based gamma-secretase inhibitors.

Andrew P Owens1, Alan Nadin, Adam C Talbot, Earl E Clarke, Timothy Harrison, Huw D Lewis, Michael Reilly, Jonathan D J Wrigley, José L Castro.   

Abstract

In this paper, we describe the development of a novel series of high affinity, orally bioavailable 3-amino-1,4 benzodiazepine-based gamma-secretase inhibitors for the potential treatment of Alzheimer's disease. We disclose structure-activity relationships based around the 1, 3 and 5 positions of the benzodiazepine core structure.

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Year:  2003        PMID: 14592525     DOI: 10.1016/j.bmcl.2003.07.031

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Drug discovery for Alzheimer's disease: the end of the beginning.

Authors:  Lorenzo M Refolo; Howard M Fillit
Journal:  J Mol Neurosci       Date:  2004       Impact factor: 3.444

2.  Three-dimensional quantitative structure-activity relationship (3D-QSAR) studies of various benzodiazepine analogues of gamma-secretase inhibitors.

Authors:  Tarnvir Sammi; Om Silakari; Muttineni Ravikumar
Journal:  J Mol Model       Date:  2008-12-06       Impact factor: 1.810

Review 3.  BACE and gamma-secretase characterization and their sorting as therapeutic targets to reduce amyloidogenesis.

Authors:  Neville Marks; Martin J Berg
Journal:  Neurochem Res       Date:  2009-09-17       Impact factor: 3.996

  3 in total

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