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吡咯并噁唑烷衍生物对 的抑制活性。

Inhibitory Activity of Pyrroloisoxazolidine Derivatives against .

机构信息

School of Pharmacy, Nantong University, Nantong 226001, China.

Department of Dermatology and Venereology, Affiliated Hospital of Nantong University, Nantong 226001, China.

出版信息

Biomed Res Int. 2021 Mar 13;2021:8889247. doi: 10.1155/2021/8889247. eCollection 2021.

Abstract

The obligate intracellular bacterium 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 in a dose-dependent manner . Among them, compounds 1 and 2 exhibited the strongest inhibitory activity with IC values from 7.25 to 9.73 M. The compounds disturbed the whole intracellular life cycle of , 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.

摘要

专性细胞内细菌是一组全球性的人类病原体,可导致严重的生殖问题。频繁的临床治疗失败促进了新型抗衣原体药物的发展。在这里,我们首次报道了一组吡咯并异噁唑烷抑制的 ,其呈剂量依赖性。其中,化合物 1 和 2 表现出最强的抑制活性,IC 值为 7.25 至 9.73 μM。这些化合物扰乱了 的整个细胞内生命周期,主要针对中网状体增殖阶段。此外,这些化合物通过在高浓度时降低原体感染力,部分抑制了衣原体感染。我们的研究结果表明,吡咯并异噁唑烷衍生物具有作为抗衣原体药物开发有前途的先导分子的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b6d/7984888/5fd2a12cf579/BMRI2021-8889247.001.jpg

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