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.
Claims5
A pharmaceutical composition comprising a pharmaceutically acceptable carrier, excipient or diluent and one or more small molecules represented by the formula:
- wherein n is 0, 1 or 2;
- Y is O, S or CH2;
- wherein the aryl ring substituent Z represents single or multiple substituents,
- wherein when Z represents a single substituent Z is located at the ortho, meta or para position and when Z represents multiple substituents, the substituents are located at any combination of the ortho, meta or para positions, and wherein Z is selected from the group consisting of halogen, hydroxyl, alkoxyl, cyano, nitro, amido, acetamido, amino, alkylamino, aryl, heteroaryl, acyl, alkyl, cycloalkyl, sulfonamide, and alkyl sulfonamide.
Dependencies are inferred from the claim text.