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    HETEROCYCLIC INHIBITORS OF BACTERIAL PEPTIDYL TRNA HYDROLASE AND USES THEREOF
    2.
    发明申请
    HETEROCYCLIC INHIBITORS OF BACTERIAL PEPTIDYL TRNA HYDROLASE AND USES THEREOF 审中-公开
    细菌肽类TRNA水解物的杂环抑制剂及其用途

    公开(公告)号：US20100069380A1

    公开(公告)日：2010-03-18

    申请号：US12441929

    申请日：2007-09-21

    申请人： Soongyu Choi ,  Arthur Branstrom ,  Scott A. Gothe ,  Richard Lipman ,  Tamil Arasu ,  Richard G. Wilde

    发明人： Soongyu Choi ,  Arthur Branstrom ,  Scott A. Gothe ,  Richard Lipman ,  Tamil Arasu ,  Richard G. Wilde

    IPC分类号： C07D491/052 ,  A61K31/5377 ,  A61K31/4741 ,  C07D491/22 ,  C07D491/16 ,  A61P31/04 ,  A61K31/4743 ,  A61K31/506 ,  C07D491/147 ,  C07D491/153 ,  A61K31/4375

    CPC分类号： C07D417/04 ,  C07D413/14 ,  C07D417/14 ,  C07D419/14 ,  C07D487/04

    摘要： Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for screening and identifying compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase. In particular, provided herein are assays for the identification of compounds that inhibit or reduce the activity of a bacterial peptidyl tRNA hydrolase. The methods provided herein provide a simple, sensitive assay for high-throughput screening of libraries of compounds to identify pharmaceutical leads useful for preventing, treating, and managing a bacterial infection or one or more symptoms thereof. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions.

    摘要翻译： 本文提供调节细菌肽基tRNA水解酶的活性的化合物，包括组合物和包含该化合物的剂型。 本文还提供了筛选和鉴定调节细菌肽基tRNA水解酶活性的化合物的方法。 特别地，本文提供了用于鉴定抑制或降低细菌肽基tRNA水解酶的活性的化合物的测定法。 本文提供的方法提供了一种用于高通量筛选化合物文库的简单敏感测定，以鉴定可用于预防，治疗和管理细菌感染或其一种或多种症状的药物引线。 本文还提供了用于预防或抑制细菌增殖的方法以及使用这些化合物和组合物预防，治疗和/或控制细菌感染的方法。