US Government As Represented by the Secretary of the Army

Other

United States Government As Represented by the Secretary of the United States Army and the U.S. Army Medical Research & Materiel Command

Rick Gussio

Sina Bavari

James C Burnett

Rekha G Panchal

Laurent Meijer

Edward A Sausville

James J Schmidt

Conrad Kunick

Tam Nguyen

Ravi Kumar Jalluri

Ann Hermone

Daniel W Zaharevitz

Disclosed herein are methods of inhibiting, reducing or preventing growth of or destroying bacteria of at least one bacterial strain which comprises contacting the bacteria with the compounds disclosed herein. Also disclosed are methods of treating, inhibiting or preventing an infection or intoxication caused by bacteria of at least one bacterial strain in a subject and pharmaceutical and cosmetic compositions comprising the compounds disclosed herein.

Broad spectrum antibacterial compounds

Disclosed herein are methods of inhibiting the activity of Botulinum neurotoxin A metalloprotease with the compounds disclosed herein. Also disclosed are methods of treating, inhibiting or preventing intoxication caused by bacteria of at least one bacterial strain in a subject, and pharmaceutical and cosmetic compositions comprising the compounds disclosed herein.

Small molecule inhibitors of botulinum neurotoxins

Disclosed herein is a pharmacophore model for inhibiting anthrax lethal factor protease activity which comprises a first aromatic center A, a second aromatic center B, a first polar center C, a second polar center D, a third polar center E, and a neutral linker F. Also disclosed are small molecules fitting the pharmacophore model and compositions and methods of using thereof.

Inhibition of anthrax lethal factor protease

Disclosed herein is a pharmacophore model for inhibiting Botulinum neurotoxin A metalloprotease activity which comprises a first plane A, a second plane B, a first hydrophobic moiety C, a second hydrophobic moiety D and a positive ionizable substituent E. The pharmacophore model may further comprise a heteroatom in the first plane A. In some embodiments, the distance between the center of the first plane A and the center of the second plane B is about 6.5 to about 9.5 &#x212b;. In some embodiments, the distance between the center of the first hydrophobic moiety C and the center of the second hydrophobic moiety D is about 8.0 to about 16.0 &#x212b;. In some embodiments, the distance between the center of the first plane to the center of the first hydrophobic moiety C is about 3.0 to about 5.0 &#x212b;. In some embodiments, the distance between the center of the second plane to the center of the second hydrophobic moiety C is about 3.0 to about 5.0 &#x212b;. In some embodiments, the distance between the center of the first plane to the center of the positive ionizable substituent is about 6.5 to about 9.5 &#x212b;.

Small molecules and a pharmacophore model for inhibition of botulinum toxin and methods of making and using thereof

Fused azepinone cyclin dependent kinase inhibitors

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Frederick, MD, United States of America

Rick Gussio