Affinium Pharmaceuticals, Inc.

Walter E Dewolf, Jr

Mark Andrew Seefeld

William Henry Miller

Kenneth Allen Newlander

Irene Nijole Uzinskas

Dalia R Jakas

Nicola Gail Wallis

Howard Kallender

David John Payne

John Timothy Lonsdale

Joshua M West

David G Tew

Shannon L Reed

Martin Brandt

Paul M Keller

Arunbhai H Patel

Compounds of the Formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.

FAB I inhibitors

Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.

Fab I inhibitors

The invention provides methods for using agonists and antagonists of FabK polypeptides, particularly to modulate the metabolism of bacteria or to treat bacterial infection.

Methods of agonizing and antagonizing FabK

Provided is a screening method for compounds affecting fatty acid biosynthesis, the method comprising: providing a reaction mixture comprising: an acyl carrier moiety or enzymes and precursors sufficient to generate the acyl carrier moiety; a bacterial enzymatic pathway comprising at least two consecutively acting enzymes selected from the group consisting of: malonyl-CoA:ACP transacylase, beta-ketoacyl-ACP synthase III, NADPH dependent beta-ketoacyl-ACP reductase, beta-hydroxylacyl-ACP dehydrase and enoyl-ACP reductase; and substrates and cofactors required for the operation of the enzymes; contacting the reaction mixture with a prospective bioactive agent; conducting a high throughput measurement of the activity of the enzymatic pathway; and determining if the contacting altered the activity of the enzymatic pathway.

High throughput screening method for biological agents affecting fatty acid biosynthesis

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Glenmoore, PA, United States of America

Walter E Dewolf, Jr