使用Biotage Isolera快速纯化液相制备色谱为设计新的抗结核药物探索解旋酶ATPase结构 by Biotage Isolera耐士科技

2015/02/12   下载量： 10 次

方案摘要

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应用领域 制药/生物制药
检测样本 化药新药研发
检测项目 其他>方法开发
参考标准 GB/T 8****

Gyrase ATPase domain, the pharmaceutical underexploited segment of DNA gyrase, the sole Type II topoisomerase present in Mycobacterium tuberculosis represents an attractive target for anti-tubercular drug discovery. Here we report, the development of a novel series of MTB DNA gyraseB inhibitor identified through a medium throughput screening (MTS) of BITS in-house chemical library (3000 compounds). The MTS hit was further remodeled by chemical synthesis to identify the most potent analogue 27 exhibiting an in vitro gyrB inhibitory IC50 of 0.15 lM. The series also demonstrated well correlating gyrase super coiling activity and in vitro anti-mycobacterial potency against MTB H37Rv strain. Furthermore the compounds displayed good safety profile in their subsequent cytotoxicity and hERG toxicity evaluations, to be worked out from a pharmaceutical point of view as potential anti-tubercular agents.

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上一篇 耐士科技：使用Biotage Isolera快速纯化液相制备色谱从库拉索芦荟叶皮提取天然的磷酸二酯酶抑制剂by耐士科技
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上海鑫欣生物科技有限公司
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