Literature DB >> 19660943

Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline gamma-secretase inhibitors.

Anh P Truong1, Danielle L Aubele, Gary D Probst, Martin L Neitzel, Chris M Semko, Simeon Bowers, Darren Dressen, Roy K Hom, Andrei W Konradi, Hing L Sham, Albert W Garofalo, Pamela S Keim, Jing Wu, Michael S Dappen, Karina Wong, Erich Goldbach, Kevin P Quinn, John-Michael Sauer, Elizabeth F Brigham, William Wallace, Lan Nguyen, Susanna S Hemphill, Michael P Bova, Frédérique Bard, Ted A Yednock, Guriqbal Basi.   

Abstract

In this Letter, we report our strategy to design potent and metabolically stable gamma-secretase inhibitors that are efficacious in reducing the cortical Abetax-40 levels in FVB mice via a single PO dose.

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Year:  2009        PMID： 19660943     DOI： 10.1016/j.bmcl.2009.07.092

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


  4 in total

Review 1.  ACS chemical neuroscience molecule spotlight on ELND006: another γ-secretase inhibitor fails in the clinic.

Authors:  Corey R Hopkins
Journal:  ACS Chem Neurosci       Date:  2011-06-15       Impact factor: 4.418

2.  Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease.

Authors:  Guriqbal S Basi; Susanna Hemphill; Elizabeth F Brigham; Anna Liao; Danielle L Aubele; Jeanne Baker; Robin Barbour; Michael Bova; Xiao-Hua Chen; Michael S Dappen; Tovah Eichenbaum; Erich Goldbach; Jon Hawkinson; Rose Lawler-Herbold; Kang Hu; Terence Hui; Jacek J Jagodzinski; Pamela S Keim; Dora Kholodenko; Lee H Latimer; Mike Lee; Jennifer Marugg; Matthew N Mattson; Scott McCauley; James L Miller; Ruth Motter; Linda Mutter; Martin L Neitzel; Huifang Ni; Lan Nguyen; Kevin Quinn; Lany Ruslim; Christopher M Semko; Paul Shapiro; Jenifer Smith; Ferdie Soriano; Balazs Szoke; Kevin Tanaka; Pearl Tang; John A Tucker; Xiacong Michael Ye; Mei Yu; Jing Wu; Ying-Zi Xu; Albert W Garofalo; John Michael Sauer; Andrei W Konradi; Daniel Ness; George Shopp; Michael A Pleiss; Stephen B Freedman; Dale Schenk
Journal:  Alzheimers Res Ther       Date:  2010-12-29       Impact factor: 6.982

3.  Sulfur-containing therapeutics in the treatment of Alzheimer's disease.

Authors:  Haizhou Zhu; Venkateshwara Dronamraju; Wei Xie; Swati S More
Journal:  Med Chem Res       Date:  2021-01-15       Impact factor: 1.965

4.  Chronic γ-secretase inhibition reduces amyloid plaque-associated instability of pre- and postsynaptic structures.

Authors:  S Liebscher; R M Page; K Käfer; E Winkler; K Quinn; E Goldbach; E F Brigham; D Quincy; G S Basi; D B Schenk; H Steiner; T Bonhoeffer; C Haass; M Meyer-Luehmann; M Hübener
Journal:  Mol Psychiatry       Date:  2013-09-24       Impact factor: 15.992
  4 in total

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