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Sansanmycin natural product analogues as potent and selective anti-mycobacterials that inhibit lipid I biosynthesis.

机译:Sansanmycin天然产物类似物可作为有效的和选择性的抗分枝杆菌药,可抑制脂质I的生物合成。

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摘要

Tuberculosis (TB) is responsible for enormous global morbidity and mortality, and current treatment regimens rely on the use of drugs that have been in use for more than 40 years. Owing to widespread resistance to these therapies, new drugs are desperately needed to control the TB disease burden. Herein, we describe the rapid synthesis of analogues of the sansanmycin uridylpeptide natural products that represent promising new TB drug leads. The compounds exhibit potent and selective inhibition of Mycobacterium tuberculosis, the etiological agent of TB, both in vitro and intracellularly. The natural product analogues were also shown to be nanomolar inhibitors of Mtb phospho-MurNAc-pentapeptide translocase, the enzyme responsible for the synthesis of lipid I in mycobacteria. This work lays the foundation for the development of uridylpeptide natural product analogues as new TB drug candidates that operate through the inhibition of peptidoglycan biosynthesis.
机译:结核病(TB)导致巨大的全球发病率和死亡率,目前的治疗方案依赖使用已使用40多年的药物。由于对这些疗法的广泛抵抗,迫切需要新药来控制结核病负担。在本文中,我们描述了代表有希望的新结核病药物线索的Sansanmycin uridylpeptide天然产物类似物的快速合成。这些化合物在体外和细胞内均表现出对结核分枝杆菌(结核病的病原体)的有效和选择性抑制作用。天然产物类似物也显示为Mtb磷酸-MurNAc-五肽转位酶的纳摩尔抑制剂,该酶负责在分枝杆菌中合成脂质I。这项工作为开发尿肽天然产物类似物奠定了基础,后者是通过抑制肽聚糖生物合成起作用的新型结核病候选药物。

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