Small molecule antagonists of bacterial quorum-sensing receptors
AssigneeThe Trustees of Princeton University
InventorsBonnie L. Bassler, Lee R. Swem, Scott M. Ulrich, Colleen T. O'Loughlin
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Abstract
A novel small molecule antagonizes two types of acyl homoserine lactone receptors: membrane-bound and cytoplasmic. A focused library of analogs and derivatives of the original antagonist was synthesized. Analog and derivative molecules harbor a range of activities. The novel small molecule and most potent antagonist protects the eukaryote Caenorhabditis elegans from quorum-sensing-mediated killing by the bacterial pathogen Chromobacterium violaceum. The saving of C. elegans demonstrates the use of these molecules as small molecule antimicrobials.
Claims10
A small molecule analog of 4-(4-chloro-2-methylphenoxy)-N-(2-oxotetrahydrothiophen-3-yl)butanamide wherein said small molecule is represented by the formula:
- wherein X is O or S;
- n is 0, 1 or 2;
- Y is O, S or CH2;
- and Z is a halogen, hydroxyl, alkoxyl, cyano, nitro, amido, acetamido, amino, alkylamino, aryl, heteroaryl, acyl, alkyl, cycloalkyl, sulfonamide, alkyl sulfonamide or a combination thereof;
- and
- wherein Z is located at the ortho, meta or para position or at a combination thereof.
Dependencies are inferred from the claim text.