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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Identification of benzothiazinones containing an oxime functional moiety as new anti-tuberculosis agents
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Identification of benzothiazinones containing an oxime functional moiety as new anti-tuberculosis agents

机译：鉴定含有肟官能部分的苯并噻唑酮作为新的抗结核剂

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摘要

A series of benzothiazinones (BTZs) containing an oxime moiety, based on the structure of ZR-10 discovered in our lab, were designed and synthesized. Most of the compounds with alkoxyimino groups attached to the piperazine or cyclohexyl ring of PBTZ169, exhibit excellent in vitro activity against both drug-sensitive and clinically isolated multidrug-resistant Mycobacterium tuberculosis (MTB) strains (MIC: < 0.016-0.037 mu g/mL) and low cell cytotoxicity. Two close PBTZ169-analogues 3a and 3b with proper ADME/T and PK properties show potent in vivo efficacy in an acute mouse model of tuberculosis. Compound 3a is under evaluation as a potential clinical candidate for treatment of tuberculosis. (C) 2019 Elsevier Masson SAS. All rights reserved.
机译：设计并合成了基于我们实验室中发现的ZR-10结构的含有肟部分的苯并噻嗪酮（BTZ）。 大多数用附着于PBTZ169的哌嗪或环己烯环的烷氧基亚氨基的大多数化合物，对药物敏感和临床分离的多药分枝杆菌（MTB）菌株的含量优异的体外活性（MIC：<0.016-0.037μg/ ml） ）和低细胞细胞毒性。 两个紧密的PBTZ169 - 类似物3A和3B，具有适当的ADME / T和PK特性，表现出急性小鼠结核病模型的体内疗效。 化合物3a是在评价中作为治疗结核病的潜在临床候选者。 （c）2019年Elsevier Masson SAS。 版权所有。

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  • 作者

    Wang Apeng; Lv Kai; Tao Zeyu; Gu Jian; Fu Lei; Liu Mingliang; Wan Baojie; Franzblau Scott G.; Ma Chao; Ma Xican; Han Bing; Wang Aoyu; Xu Shijie; Lu Yu;

  • 作者单位

    Chinese Acad Med Sci &

    Peking Union Med Coll Inst Med Biotechnol Beijing 100050 Peoples R China;

    Chinese Acad Med Sci &

    Peking Union Med Coll Inst Med Biotechnol Beijing 100050 Peoples R China;

    Chinese Acad Med Sci &

    Peking Union Med Coll Inst Med Biotechnol Beijing 100050 Peoples R China;

    Southwest Minzu Univ Coll Pharm Chengdu 610041 Sichuan Peoples R China;

    Med Univ Beijing TB &

    Thorac Tumor Res Inst Beijing Key Lab Drug Resistance TB Res Beijing Chest;

    Chinese Acad Med Sci &

    Peking Union Med Coll Inst Med Biotechnol Beijing 100050 Peoples R China;

    Univ Illinois Coll Pharm Inst TB Res Chicago IL 60612 USA;

    Univ Illinois Coll Pharm Inst TB Res Chicago IL 60612 USA;

    Chinese Acad Med Sci &

    Peking Union Med Coll Inst Med Biotechnol Beijing 100050 Peoples R China;

    Chinese Acad Med Sci &

    Peking Union Med Coll Inst Med Biotechnol Beijing 100050 Peoples R China;

    Chinese Acad Med Sci &

    Peking Union Med Coll Inst Med Biotechnol Beijing 100050 Peoples R China;

    Chinese Acad Med Sci &

    Peking Union Med Coll Inst Med Biotechnol Beijing 100050 Peoples R China;

    Chinese Acad Med Sci &

    Peking Union Med Coll Inst Med Biotechnol Beijing 100050 Peoples R China;

    Med Univ Beijing TB &

    Thorac Tumor Res Inst Beijing Key Lab Drug Resistance TB Res Beijing Chest;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 药学;
  • 关键词

    Benzothiazinones; Oximes; Antimycobacterial activity; Synthesis;

    机译：苯并噻唑酮;肟;抗致细胞活动;合成;

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