Small Molecule Lipid II Inhibitors
    7.
    发明申请

    公开(公告)号:US20190002426A1

    公开(公告)日:2019-01-03

    申请号:US16064276

    申请日:2016-12-20

    Abstract: Newly synthesized derivatives of BAS00127538 have been discovered to possess antibiotic activity and to combat resistant bacterial strains. Compounds and pharmaceutical compositions containing these compounds are described, and are based on a generic scaffold structure. Synthetic methods and methods of using the compounds also are described. Preferred compound 6jc48-1 ((E)-2,4-bis(4-bromophenyl)-6-(4-(dimethyl-amino)styryl)pyrylium boron tetrafluoride salt) binds to Lipid II with high affinity, has markedly reduced cytotoxicity than BAS00127538, and retains activity against drug-resistant strains of Enterococci. It is stable in plasma, has dramatically improved pharmacokinetic and pharmacodynamics properties, and possesses in vivo efficacy in a mouse model of sepsis.

    Method for detecting a target substance in a sample, utilizing pyrylium
compound
    9.
    发明授权
    Method for detecting a target substance in a sample, utilizing pyrylium compound 失效
    利用吡喃鎓化合物检测样品中目标物质的方法

    公开(公告)号:US6156506A

    公开(公告)日:2000-12-05

    申请号:US825586

    申请日:1997-04-01

    CPC classification number: G01N33/582 C07D309/34 C12Q1/6818 G01N33/533

    Abstract: A method for detecting a target substance in a sample comprises the steps of providing at least two reagents which can form a reaction system for causing changes as the result of an interaction therebetween the interaction being caused only when the target substance is present in the sample, reacting the reagents with the target substance, and measuring the resulting changes based on the interaction, wherein at least one of the reagents forming the reaction system is selected from specific pyrylium compounds.

    Abstract translation: 用于检测样品中目标物质的方法包括以下步骤:提供至少两种试剂,其可以形成用于引起作为其之间相互作用的结果的变化的反应体系,所述相互作用仅在样品中存在目标物质时引起 使试剂与目标物质反应,并根据相互作用测量所得的变化,其中形成反应体系的至少一种试剂选自特定的吡喃鎓化合物。

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