Literature DB >> 16338135

The discovery of a potent and selective lethal factor inhibitor for adjunct therapy of anthrax infection.

Yusheng Xiong1, Judyann Wiltsie, Andrea Woods, Jian Guo, James V Pivnichny, Wei Tang, Alka Bansal, Richard T Cummings, Barry R Cunningham, Arthur M Friedlander, Cameron M Douglas, Scott P Salowe, Dennis M Zaller, Edward M Scolnick, Dennis M Schmatz, Kenneth Bartizal, Jeffrey D Hermes, Malcolm MacCoss, Kevin T Chapman.   

Abstract

A potent and selective anthrax LF inhibitor 40, (2R)-2-[(4-fluoro-3-methylphenyl)sulfonylamino]-N-hydroxy-2-(tetrahydro-2H-pyran-4-yl)acetamide, was identified through SAR study of a high throughput screen lead. It has an IC50 of 54 nM in the enzyme assay and an IC50 of 210 nM in the macrophage cytotoxicity assay. Compound 40 is also effective in vivo in several animal model studies.

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Year:  2005        PMID: 16338135     DOI: 10.1016/j.bmcl.2005.10.088

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


  20 in total

1.  Thioamide hydroxypyrothiones supersede amide hydroxypyrothiones in potency against anthrax lethal factor.

Authors:  Arpita Agrawal; César Augusto F de Oliveira; Yuhui Cheng; Jennifer A Jacobsen; J Andrew McCammon; Seth M Cohen
Journal:  J Med Chem       Date:  2009-02-26       Impact factor: 7.446

2.  In vivo efficacy of beta-cyclodextrin derivatives against anthrax lethal toxin.

Authors:  Mahtab Moayeri; Tanisha M Robinson; Stephen H Leppla; Vladimir A Karginov
Journal:  Antimicrob Agents Chemother       Date:  2008-03-31       Impact factor: 5.191

3.  A novel pharmacophore model for the design of anthrax lethal factor inhibitors.

Authors:  Hongbin Yuan; Sherida L Johnson; Li-Hsing Chen; Jun Wei; Maurizio Pellecchia
Journal:  Chem Biol Drug Des       Date:  2010-06-21       Impact factor: 2.817

Review 4.  An overview of investigational toxin-directed therapies for the adjunctive management of Bacillus anthracis infection and sepsis.

Authors:  Lernik Ohanjanian; Kenneth E Remy; Yan Li; Xizhong Cui; Peter Q Eichacker
Journal:  Expert Opin Investig Drugs       Date:  2015-04-28       Impact factor: 6.206

5.  Highly predictive support vector machine (SVM) models for anthrax toxin lethal factor (LF) inhibitors.

Authors:  Xia Zhang; Elizabeth Ambrose Amin
Journal:  J Mol Graph Model       Date:  2015-11-17       Impact factor: 2.518

6.  Ligand-induced expansion of the S1' site in the anthrax toxin lethal factor.

Authors:  Kimberly M Maize; Elbek K Kurbanov; Rodney L Johnson; Elizabeth Ambrose Amin; Barry C Finzel
Journal:  FEBS Lett       Date:  2015-11-11       Impact factor: 4.124

7.  Small molecule inhibitors of anthrax lethal factor toxin.

Authors:  John D Williams; Atiyya R Khan; Steven C Cardinale; Michelle M Butler; Terry L Bowlin; Norton P Peet
Journal:  Bioorg Med Chem       Date:  2013-11-13       Impact factor: 3.641

8.  Identification of novel non-hydroxamate anthrax toxin lethal factor inhibitors by topomeric searching, docking and scoring, and in vitro screening.

Authors:  Ting-Lan Chiu; Jonathan Solberg; Satish Patil; Todd W Geders; Xia Zhang; Subhashree Rangarajan; Rawle Francis; Barry C Finzel; Michael A Walters; Derek J Hook; Elizabeth A Amin
Journal:  J Chem Inf Model       Date:  2009-12       Impact factor: 4.956

9.  Novel inhibitors of anthrax edema factor.

Authors:  Deliang Chen; Milind Misra; Laurie Sower; Johnny W Peterson; Glen E Kellogg; Catherine H Schein
Journal:  Bioorg Med Chem       Date:  2008-06-28       Impact factor: 3.641

10.  Defensive strategies of Bacillus anthracis that promote a fatal disease.

Authors:  Jeremy Mogridge
Journal:  Drug Discov Today Dis Mech       Date:  2007
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