4.5 Article

Antidotes to anthrax lethal factor intoxication. Part 1: Discovery of potent lethal factor inhibitors with in vivo efficacy

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 22, Pages 6850-6853

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.08.058

Keywords

Anthrax; Lethal factor; Inhibitor; Small molecule

Funding

  1. National Institutes of Health [R44 AI052587]
  2. NIH, National Institute of Allergy and Infectious Diseases

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Sub-nanomolar small molecule inhibitors of anthrax lethal factor have been identified using SAR and Merck L915 (4) as a model compound. One of these compounds (16) provided 100% protection in a rat lethal toxin model of anthrax disease. (C) 2010 Elsevier Ltd. All rights reserved.

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