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公开(公告)号：US09751851B2
公开(公告)日：2017-09-05
申请号：US15023279
申请日：2014-09-19
申请人： THE TRUSTEES OF PRINCETON UNIVERSITY , Bonnie L. Bassler , Martin F. Semmelhack , Knut Drescher , Albert Siryaporn , Laura C. Miller , Colleen T. O'Loughlin
发明人： Bonnie L. Bassler , Martin F. Semmelhack , Knut Drescher , Albert Siryaporn , Laura C. Conrad-Miller , Colleen T. O'Loughlin
IPC分类号： C07D333/32 , A61K45/06 , C07D213/75 , C07D239/42 , C07D239/47 , C07D307/33
CPC分类号： C07D333/32 , A61K45/06 , C07D213/75 , C07D239/42 , C07D239/47 , C07D307/33
摘要： Antivirulence strategies to combat Pseudomonas aeruginosa, are described. One strategy encompasses synthesis of a series of compounds that inhibit the production of pyocyanin, a redox-active virulence factor produced by this pathogen. A related strategy encompasses synthesis of compounds that inhibit the two P. aeruginosa quorum-sensing receptors, LasR and RhlR, inhibit production of pyocyanin, and inhibit biofilm formation.
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2.发明申请公开(公告)号：US20160368892A1
公开(公告)日：2016-12-22
申请号：US15023279
申请日：2014-09-19
申请人： Bonnie L. BASSLER , Martin F. SEMMELHACK , Knut DRESCHER , Albert SIRYAPORN , Laura C. MILLER , Colleen T. O"LOUGHLIN , THE TRUSTEES OF PRINCETON UNIVERSITY
发明人： Bonnie L. Bassler , Martin F. Semmelhack , Knut Drescher , Albert Siryaporn , Laura C. Conrad-Miller , Colleen T. O'Loughlin
IPC分类号： C07D333/32 , C07D213/75 , C07D307/33
CPC分类号： C07D333/32 , A61K45/06 , C07D213/75 , C07D239/42 , C07D239/47 , C07D307/33
摘要： Antivirulence strategies to combat Pseudomonas aeruginosa, are described. One strategy encompasses synthesis of a series of compounds that inhibit the production of pyocyanin, a redox-active virulence factor produced by this pathogen. A related strategy encompasses synthesis of compounds that inhibit the two P. aeruginosa quorum-sensing receptors, LasR and RhlR, inhibit production of pyocyanin, and inhibit biofilm formation.
摘要翻译： 描述了防治铜绿假单胞菌的防毒素策略。 一种策略包括合成一系列化合物，其抑制由该病原体产生的氧化还原活性毒力因子的绿脓素的产生。 相关的策略包括合成抑制两种铜绿假单胞菌群体感受受体的化合物，LasR和RhIR抑制绿脓杆菌的产生，并抑制生物膜形成。
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公开(公告)号：US08772331B2
公开(公告)日：2014-07-08
申请号：US13550961
申请日：2012-07-17
IPC分类号： A61K31/381 , C07D333/32
CPC分类号： A61K31/365 , A01N43/08 , A01N43/10 , A01N43/16 , A01N43/18 , A61K31/341 , A61K31/381 , 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.
摘要翻译： 一种新的小分子拮抗两种类型的酰基高丝氨酸内酯受体：膜结合和细胞质。 合成了原始拮抗剂类似物和衍生物的重点文库。 模拟和衍生分子具有一系列活动。 新型小分子和最有效的拮抗剂通过细菌病原体Chromobacterium violaceum从群体感应介导的杀伤中保护真核生物线虫。 秀丽隐杆线虫的保存证明了这些分子作为小分子抗菌药物的用途。
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公开(公告)号：US20140275232A1
公开(公告)日：2014-09-18
申请号：US14288984
申请日：2014-05-28
CPC分类号： A61K31/365 , A01N43/08 , A01N43/10 , A01N43/16 , A01N43/18 , A61K31/341 , A61K31/381 , 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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公开(公告)号：US20100160423A1
公开(公告)日：2010-06-24
申请号：US12643574
申请日：2009-12-21
IPC分类号： A61K31/381 , A61K31/341 , C07D333/36 , C07D307/33 , A61P31/04 , A01N43/10 , A01N43/08 , A01P1/00
CPC分类号： A61K31/365 , A01N43/08 , A01N43/10 , A01N43/16 , A01N43/18 , A61K31/341 , A61K31/381 , 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.
摘要翻译： 一种新的小分子拮抗两种类型的酰基高丝氨酸内酯受体：膜结合和细胞质。 合成了原始拮抗剂类似物和衍生物的重点文库。 模拟和衍生分子具有一系列活动。 新型小分子和最有效的拮抗剂通过细菌病原体Chromobacterium violaceum从群体感应介导的杀伤中保护真核生物线虫。 秀丽隐杆线虫的保存证明了这些分子作为小分子抗菌药物的用途。
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公开(公告)号：US20140024707A1
公开(公告)日：2014-01-23
申请号：US13550961
申请日：2012-07-17
IPC分类号： A01N43/08 , A61K31/365
CPC分类号： A61K31/365 , A01N43/08 , A01N43/10 , A01N43/16 , A01N43/18 , A61K31/341 , A61K31/381 , 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.
摘要翻译： 一种新的小分子拮抗两种类型的酰基高丝氨酸内酯受体：膜结合和细胞质。 合成了原始拮抗剂类似物和衍生物的重点文库。 模拟和衍生分子具有一系列活动。 新型小分子和最有效的拮抗剂通过细菌病原体Chromobacterium violaceum从群体感应介导的杀伤中保护真核生物线虫。 秀丽隐杆线虫的保存证明了这些分子作为小分子抗菌药物的用途。
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公开(公告)号：US08247443B2
公开(公告)日：2012-08-21
申请号：US12643574
申请日：2009-12-21
IPC分类号： A61K31/381 , C07D333/32
CPC分类号： A61K31/365 , A01N43/08 , A01N43/10 , A01N43/16 , A01N43/18 , A61K31/341 , A61K31/381 , 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.
摘要翻译： 一种新的小分子拮抗两种类型的酰基高丝氨酸内酯受体：膜结合和细胞质。 合成了原始拮抗剂类似物和衍生物的重点文库。 模拟和衍生分子具有一系列活动。 新型小分子和最有效的拮抗剂通过细菌病原体Chromobacterium violaceum从群体感应介导的杀伤中保护真核生物线虫。 秀丽隐杆线虫的保存证明了这些分子作为小分子抗菌药物的用途。
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8.发明申请公开(公告)号：US20150191765A1
公开(公告)日：2015-07-09
申请号：US14589845
申请日：2015-01-05
发明人： Bonnie L. Bassler , Howard A. Stone , Martin F. Semmelhack , Knut Drescher , Yi Shen , Colleen T. O'Loughlin , Laura C. Miller
摘要： The present invention relates to a method of measuring biofilms and/or biofilm streamers, wherein the method comprises a system that has at least one channel and a biofilm streamer promotion element, a fluid capable of moving along the channel, wherein the fluid has a flow driven by a controlled pressure; and a measuring element capable of measuring a flow rate of the fluid through the channel. Additionally, method of screening for compound(s) that promote and/or inhibit biofilm and/or biofilm streamers using this system are also contemplated. Uses of the system, methods and identified compounds are contemplated for medical and/or industrial environments.
摘要翻译： 本发明涉及测量生物膜和/或生物膜拖缆的方法，其中所述方法包括具有至少一个通道和生物膜拖缆促进元件的系统，能够沿着通道移动的流体，其中流体具有流动 由受控压力驱动; 以及能够测量通过通道的流体的流量的测量元件。 此外，还考虑了使用该系统筛选促进和/或抑制生物膜和/或生物膜拖缆的化合物的方法。 用于医疗和/或工业环境的系统，方法和鉴定的化合物的用途。
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公开(公告)号：US09468624B2
公开(公告)日：2016-10-18
申请号：US14739841
申请日：2015-06-15
IPC分类号： A01N43/06 , A61K31/38 , C07D333/36 , C07D333/42 , A61K31/365 , A01N43/08 , A01N43/10 , A01N43/16 , A01N43/18 , A61K31/341 , A61K31/381 , C07D307/33
CPC分类号： A61K31/365 , A01N43/08 , A01N43/10 , A01N43/16 , A01N43/18 , A61K31/341 , A61K31/381 , 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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公开(公告)号：US20150306067A1
公开(公告)日：2015-10-29
申请号：US14739841
申请日：2015-06-15
IPC分类号： A61K31/365
CPC分类号： A61K31/365 , A01N43/08 , A01N43/10 , A01N43/16 , A01N43/18 , A61K31/341 , A61K31/381 , 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.
摘要翻译： 一种新的小分子拮抗两种类型的酰基高丝氨酸内酯受体：膜结合和细胞质。 合成了原始拮抗剂类似物和衍生物的重点文库。 模拟和衍生分子具有一系列活动。 新型小分子和最有效的拮抗剂通过细菌病原体Chromobacterium violaceum从群体感应介导的杀伤中保护真核生物线虫。 秀丽隐杆线虫的保存证明了这些分子作为小分子抗菌药物的用途。
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