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Inhibitory Activity of Pyrroloisoxazolidine Derivatives against Chlamydia trachomatis

机译:吡咯烷嗪唑烷衍生物对衣原体粉碎瘤的抑制活性

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摘要

The obligate intracellular bacterium Chlamydia trachomatis is a group of worldwide human pathogens that can lead to serious reproductive problems. The frequent clinical treatment failure promoted the development of novel antichlamydial agents. Here, we firstly reported a group of pyrroloisoxazolidine-inhibited C. trachomatis in a dose-dependent manner in vitro. Among them, compounds 1 and 2 exhibited the strongest inhibitory activity with IC50 values from 7.25 to 9.73 μM. The compounds disturbed the whole intracellular life cycle of C. trachomatis, mainly targeting the middle reticulate body proliferation stages. Besides, the compounds partially inhibited the chlamydial infection by reducing elementary body infectivity at high concentration. Our findings suggest the potential of pyrroloisoxazolidine derivatives as promising lead molecules for the development of antichlamydial agents.
机译:Interacellularbacterium Chlamydia Trachomatis是一群全球人类病原体,可能导致严重的生殖问题。频繁的临床治疗失败促进了新型抗血症药的发展。在这里,我们首先在体外以剂量依赖性方式报道了一组吡咯唑异恶唑烷酰胺抑制的C.Trachomatis。其中,化合物1和2表现出具有7.25至9.73μm的IC 50值最强的抑制活性。该化合物扰乱了C. Thachomatis的整个细胞内生命周期,主要靶向中间网状体增殖阶段。此外,该化合物通过在高浓度下减少基本的体内感染性而部分地抑制衣原体感染。我们的研究结果表明吡咯唑唑唑烷衍生物作为抗暗症药物的发育的有前途的铅分子。

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