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Sci Rep：苯并噻嗪-4-硫酮，一种很有前途的治疗耐药结核病的临床前候选药

2016-11-18 xing.T MedSci原创

耐药结核病
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这些数据结合苯并噻嗪-4-硫酮的安全性和生物利用度表明SKLB-TB1001是一种很有前途的治疗耐药结核病的前临床候选药物。

全球每年死于结核病的人数近300万，中国患病人数居世界第二。由于多重耐药/广谱耐药结核病的出现，现有抗结核病药物已不能满足治愈需求，开发新的化疗药物以应对耐多药分枝杆菌结核病，这仍然是一个严重的公共卫生挑战。 

最近，来自中国四川华西医院生物治疗国家重点实验室的高超博士和余洛汀博士在Sci Rep杂志上发表研究文章，在他们的文章中DprE1酶被描述为一个有吸引力的治疗靶点有望来解决这个迫切的需求。

在该研究中，研究者已经确定了一类新的DprE1酶抑制剂-苯并噻嗪-4-硫酮-作为抗结核药。在微孔板Alamar蓝试验和细胞模型上苯并噻嗪-4-硫酮类似物SKLB-TB1001表现出了优异的抗耐多药分枝杆菌结核病特性，同时SKLB-TB1001对从临床患者分离出来的耐多药和超级耐多药菌株也是高度有效的。


SKLB-TB1001的化学结构 

重要的是，研究人员在两种药物组合测试中也没有发现任何拮抗作用，而且SKLB-TB1001和利福平（RMP）的组合被证明具有协同效应。此外，苯并噻嗪-4-硫酮在急性结核分枝杆菌感染的小鼠模型体内也表现出了优异的抗结核疗效，并明显优于BTZ043。 

这些数据结合苯并噻嗪-4-硫酮的安全性和生物利用度表明SKLB-TB1001是一种很有前途的治疗耐药结核病的临床前候选药物。

原始出处： 

Gao C, et al. Benzothiazinethione is a potent preclinical candidate for the treatment of drug-resistant tuberculosis. Sci Rep. 2016 Jul 13;6:29717.

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    2017-03-06 fangcong

    #噻嗪#

    0

  2. [GetPortalCommentsPageByObjectIdResponse(id=1643222, encodeId=23fb16432224b, content=<a href='/topic/show?id=97b840365d7' target=_blank style='color:#2F92EE;'>#噻嗪#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=33, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=40365, encryptionId=97b840365d7, topicName=噻嗪)], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=0e9523156615, createdName=fangcong, createdTime=Mon Mar 06 11:54:00 CST 2017, time=2017-03-06, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=1254018, encodeId=e5461254018b4, content=<a href='/topic/show?id=f30ae86297d' target=_blank style='color:#2F92EE;'>#结核#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=27, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=78629, encryptionId=f30ae86297d, topicName=结核)], attachment=null, authenticateStatus=null, createdAvatar=, createdBy=4dfa37, createdName=huhuaidong387, createdTime=Sun Nov 20 03:54:00 CST 2016, time=2016-11-20, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=156672, encodeId=aeee1566e228, content=脊柱结核同样值得关注！, beContent=null, objectType=article, channel=null, level=null, likeNumber=89, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=http://thirdwx.qlogo.cn/mmopen/vi_32/sp9HFtQXjmv7KvIaqDy1qMa7WNiaQhIq06LSXTojGjtTG418ibnmY9yU0VBHUhGWHgia6dk8hkUJx4zBrc2TMC6bA/132, createdBy=33051979095, createdName=黑哥哥, createdTime=Fri Nov 18 21:01:21 CST 2016, time=2016-11-18, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=156649, encodeId=811915664979, content=积分看视频, beContent=null, objectType=article, channel=null, level=null, likeNumber=1, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=, createdBy=3a6a1669343, createdName=阿玖, createdTime=Fri Nov 18 17:44:09 CST 2016, time=2016-11-18, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=156612, encodeId=d2c8156612ea, content=现在结核病又开始多起来。。, beContent=null, objectType=article, channel=null, level=null, likeNumber=84, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/ajNVdqHZLLCqgUEJ5wK4ouoGLSPnGrpRpsx3qF8s2REkzeqA3OarPBnRiaauicCtuwUh8Vk360mONiaUFeH1x22gQ/0, createdBy=93851982464, createdName=eviolet7, createdTime=Fri Nov 18 13:39:38 CST 2016, time=2016-11-18, status=1, ipAttribution=)]
    2016-11-20 huhuaidong387

    #结核#

    0

  3. [GetPortalCommentsPageByObjectIdResponse(id=1643222, encodeId=23fb16432224b, content=<a href='/topic/show?id=97b840365d7' target=_blank style='color:#2F92EE;'>#噻嗪#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=33, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=40365, encryptionId=97b840365d7, topicName=噻嗪)], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=0e9523156615, createdName=fangcong, createdTime=Mon Mar 06 11:54:00 CST 2017, time=2017-03-06, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=1254018, encodeId=e5461254018b4, content=<a href='/topic/show?id=f30ae86297d' target=_blank style='color:#2F92EE;'>#结核#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=27, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=78629, encryptionId=f30ae86297d, topicName=结核)], attachment=null, authenticateStatus=null, createdAvatar=, createdBy=4dfa37, createdName=huhuaidong387, createdTime=Sun Nov 20 03:54:00 CST 2016, time=2016-11-20, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=156672, encodeId=aeee1566e228, content=脊柱结核同样值得关注！, beContent=null, objectType=article, channel=null, level=null, likeNumber=89, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=http://thirdwx.qlogo.cn/mmopen/vi_32/sp9HFtQXjmv7KvIaqDy1qMa7WNiaQhIq06LSXTojGjtTG418ibnmY9yU0VBHUhGWHgia6dk8hkUJx4zBrc2TMC6bA/132, createdBy=33051979095, createdName=黑哥哥, createdTime=Fri Nov 18 21:01:21 CST 2016, time=2016-11-18, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=156649, encodeId=811915664979, content=积分看视频, beContent=null, objectType=article, channel=null, level=null, likeNumber=1, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=, createdBy=3a6a1669343, createdName=阿玖, createdTime=Fri Nov 18 17:44:09 CST 2016, time=2016-11-18, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=156612, encodeId=d2c8156612ea, content=现在结核病又开始多起来。。, beContent=null, objectType=article, channel=null, level=null, likeNumber=84, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/ajNVdqHZLLCqgUEJ5wK4ouoGLSPnGrpRpsx3qF8s2REkzeqA3OarPBnRiaauicCtuwUh8Vk360mONiaUFeH1x22gQ/0, createdBy=93851982464, createdName=eviolet7, createdTime=Fri Nov 18 13:39:38 CST 2016, time=2016-11-18, status=1, ipAttribution=)]
    2016-11-18 黑哥哥

    脊柱结核同样值得关注！

    0

  4. [GetPortalCommentsPageByObjectIdResponse(id=1643222, encodeId=23fb16432224b, content=<a href='/topic/show?id=97b840365d7' target=_blank style='color:#2F92EE;'>#噻嗪#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=33, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=40365, encryptionId=97b840365d7, topicName=噻嗪)], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=0e9523156615, createdName=fangcong, createdTime=Mon Mar 06 11:54:00 CST 2017, time=2017-03-06, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=1254018, encodeId=e5461254018b4, content=<a href='/topic/show?id=f30ae86297d' target=_blank style='color:#2F92EE;'>#结核#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=27, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=78629, encryptionId=f30ae86297d, topicName=结核)], attachment=null, authenticateStatus=null, createdAvatar=, createdBy=4dfa37, createdName=huhuaidong387, createdTime=Sun Nov 20 03:54:00 CST 2016, time=2016-11-20, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=156672, encodeId=aeee1566e228, content=脊柱结核同样值得关注！, beContent=null, objectType=article, channel=null, level=null, likeNumber=89, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=http://thirdwx.qlogo.cn/mmopen/vi_32/sp9HFtQXjmv7KvIaqDy1qMa7WNiaQhIq06LSXTojGjtTG418ibnmY9yU0VBHUhGWHgia6dk8hkUJx4zBrc2TMC6bA/132, createdBy=33051979095, createdName=黑哥哥, createdTime=Fri Nov 18 21:01:21 CST 2016, time=2016-11-18, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=156649, encodeId=811915664979, content=积分看视频, beContent=null, objectType=article, channel=null, level=null, likeNumber=1, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=, createdBy=3a6a1669343, createdName=阿玖, createdTime=Fri Nov 18 17:44:09 CST 2016, time=2016-11-18, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=156612, encodeId=d2c8156612ea, content=现在结核病又开始多起来。。, beContent=null, objectType=article, channel=null, level=null, likeNumber=84, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/ajNVdqHZLLCqgUEJ5wK4ouoGLSPnGrpRpsx3qF8s2REkzeqA3OarPBnRiaauicCtuwUh8Vk360mONiaUFeH1x22gQ/0, createdBy=93851982464, createdName=eviolet7, createdTime=Fri Nov 18 13:39:38 CST 2016, time=2016-11-18, status=1, ipAttribution=)]
    2016-11-18 阿玖

    积分看视频

    0

  5. [GetPortalCommentsPageByObjectIdResponse(id=1643222, encodeId=23fb16432224b, content=<a href='/topic/show?id=97b840365d7' target=_blank style='color:#2F92EE;'>#噻嗪#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=33, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=40365, encryptionId=97b840365d7, topicName=噻嗪)], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=0e9523156615, createdName=fangcong, createdTime=Mon Mar 06 11:54:00 CST 2017, time=2017-03-06, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=1254018, encodeId=e5461254018b4, content=<a href='/topic/show?id=f30ae86297d' target=_blank style='color:#2F92EE;'>#结核#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=27, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=78629, encryptionId=f30ae86297d, topicName=结核)], attachment=null, authenticateStatus=null, createdAvatar=, createdBy=4dfa37, createdName=huhuaidong387, createdTime=Sun Nov 20 03:54:00 CST 2016, time=2016-11-20, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=156672, encodeId=aeee1566e228, content=脊柱结核同样值得关注！, beContent=null, objectType=article, channel=null, level=null, likeNumber=89, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=http://thirdwx.qlogo.cn/mmopen/vi_32/sp9HFtQXjmv7KvIaqDy1qMa7WNiaQhIq06LSXTojGjtTG418ibnmY9yU0VBHUhGWHgia6dk8hkUJx4zBrc2TMC6bA/132, createdBy=33051979095, createdName=黑哥哥, createdTime=Fri Nov 18 21:01:21 CST 2016, time=2016-11-18, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=156649, encodeId=811915664979, content=积分看视频, beContent=null, objectType=article, channel=null, level=null, likeNumber=1, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=, createdBy=3a6a1669343, createdName=阿玖, createdTime=Fri Nov 18 17:44:09 CST 2016, time=2016-11-18, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=156612, encodeId=d2c8156612ea, content=现在结核病又开始多起来。。, beContent=null, objectType=article, channel=null, level=null, likeNumber=84, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://wx.qlogo.cn/mmopen/ajNVdqHZLLCqgUEJ5wK4ouoGLSPnGrpRpsx3qF8s2REkzeqA3OarPBnRiaauicCtuwUh8Vk360mONiaUFeH1x22gQ/0, createdBy=93851982464, createdName=eviolet7, createdTime=Fri Nov 18 13:39:38 CST 2016, time=2016-11-18, status=1, ipAttribution=)]
    2016-11-18 eviolet7

    现在结核病又开始多起来。。

    0