发明授权
- 专利标题: Small molecule antagonists of bacterial quorum-sensing receptors
- 专利标题(中): 小分子拮抗剂的细菌群体感应受体
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申请号: US14288984申请日: 2014-05-28
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公开(公告)号: US09084773B2公开(公告)日: 2015-07-21
- 发明人: Bonnie L. Bassler , Lee R. Swem , Scott M. Ulrich , Colleen T. O'Loughlin
- 申请人: The Trustees of Princeton University
- 申请人地址: US NJ Princeton
- 专利权人: The Trustees of Princeton University
- 当前专利权人: The Trustees of Princeton University
- 当前专利权人地址: US NJ Princeton
- 代理机构: Meagher Emanuel Laks Goldberg & Liao, LLP
- 主分类号: A61K31/381
- IPC分类号: A61K31/381 ; C07D333/32 ; A61K31/365 ; A01N43/08 ; A01N43/10 ; A01N43/16 ; A01N43/18 ; A61K31/341 ; C07D307/33 ; C07D333/36
摘要:
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.
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