Small molecule antagonists of bacterial quorum-sensing receptors

US8247443B2 · kind B2 · utility

Assignee

• THE TRUSTEES OF PRINCETON UNIVERSITY · US

Inventors

• Bonnie L. Bassler · Princeton, US
• Lee Swem · Montara, US
• Scott M. Ulrich · Brooktondale, US
• Colleen T. O'Loughlin · Princeton, US

Key dates

• Filing date: Dec 21, 2009
• Grant date: Aug 21, 2012
• Expiry date: Nov 24, 2030

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D333/36
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

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.