Literature DB >> 17764937

Thiazole-diamides as potent gamma-secretase inhibitors.

Yuhpyng L Chen1, Kevin Cherry, Michael L Corman, Charles F Ebbinghaus, Chandra B Gamlath, Dane Liston, Barbara-Anne Martin, Christine E Oborski, Barbara G Sahagan.   

Abstract

The thiazole-diamide series (1) has been identified as highly potent gamma-secretase inhibitors. Several representative compounds showed IC(50) values of <0.3 nM. The synthesis and SAR, as well as a radiolabeled synthesis of [(3)H]-2a, are described.

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Year:  2007        PMID: 17764937     DOI: 10.1016/j.bmcl.2007.08.035

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


  2 in total

1.  Substituted dithiazole piperazine benzamides as novel amyloid beta peptide reducing agents.

Authors:  Hongjie Wang; Ruizhi Wang; Madepalli K Lakshmana; Adel Nefzi
Journal:  Bioorg Med Chem Lett       Date:  2014-08-13       Impact factor: 2.823

2.  Potent s-cis-locked bithiazole correctors of DeltaF508 cystic fibrosis transmembrane conductance regulator cellular processing for cystic fibrosis therapy.

Authors:  Gui Jun Yu; Choong L Yoo; Baoxue Yang; Michael W Lodewyk; Liping Meng; Tamer T El-Idreesy; James C Fettinger; Dean J Tantillo; A S Verkman; Mark J Kurth
Journal:  J Med Chem       Date:  2008-09-13       Impact factor: 7.446

  2 in total

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