Literature DB >> 20206516

Discovery of sulfonamide-pyrazole gamma-secretase inhibitors.

Matthew N Mattson1, Martin L Neitzel, David A Quincy, Christopher M Semko, Albert W Garofalo, Pamela S Keim, Andrei W Konradi, Michael A Pleiss, Hing L Sham, Elizabeth F Brigham, Erich G Goldbach, Hongbin Zhang, John-Michael Sauer, Guriqbal S Basi.   

Abstract

Utilizing a pharmacophore hypothesis, previously described gamma-secretase inhibiting HTS hits were evolved into novel tricyclic sulfonamide-pyrazoles, with high in vitro potency, good brain penetration, low metabolic stability, and high clearance. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20206516     DOI： 10.1016/j.bmcl.2010.02.050

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


  3 in total

1.  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

2.  Lead optimization of a pyrazole sulfonamide series of Trypanosoma brucei N-myristoyltransferase inhibitors: identification and evaluation of CNS penetrant compounds as potential treatments for stage 2 human African trypanosomiasis.

Authors:  Stephen Brand; Neil R Norcross; Stephen Thompson; Justin R Harrison; Victoria C Smith; David A Robinson; Leah S Torrie; Stuart P McElroy; Irene Hallyburton; Suzanne Norval; Paul Scullion; Laste Stojanovski; Frederick R C Simeons; Daan van Aalten; Julie A Frearson; Ruth Brenk; Alan H Fairlamb; Michael A J Ferguson; Paul G Wyatt; Ian H Gilbert; Kevin D Read
Journal:  J Med Chem       Date:  2014-11-20       Impact factor: 7.446

Review 3.  Pharmaceutical and medicinal significance of sulfur (SVI)-Containing motifs for drug discovery: A critical review.

Authors:  Chuang Zhao; K P Rakesh; L Ravidar; Wan-Yin Fang; Hua-Li Qin
Journal:  Eur J Med Chem       Date:  2018-11-22       Impact factor: 6.514
  3 in total

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