衣原体
吩嗪
沙眼衣原体
微生物学
衣原体
赫拉
病菌
化学
细胞毒性
传染性
IC50型
体外
生物
病毒学
生物化学
病毒
免疫学
作者
Xiaofeng Bao,Xin Yu,Chao Xia,Ningjing Yang,Shengju Yang,Yu Zhao
出处
期刊:Letters in Drug Design & Discovery
[Bentham Science]
日期:2018-11-29
卷期号:16 (2): 174-181
被引量:2
标识
DOI:10.2174/1570180815666180518112952
摘要
Abstract: Background: Chlamydiae are widespread Gram-negative bacteria that cause a number of human diseases. Chlamydia trachomatis is the most prevalent sexually transmitted bacterial pathogen. </P><P> Methods: Fourteen novel phenazine derivatives were efficiently synthesized via Buchwald-Hartwig cross coupling reaction and Suzuki reaction from 4-bromo-1-methoxyphenazine. All the derivatives displayed antichlamydial activity with IC50 values from 1.01-19.77 µM against Chlamydia trachomatis D and L2 for inhibiting progeny formation. Results: C-4 morpholinyl 8a and C-4 phenyl phenazine 9c exhibited stronger antichlamydial activity with no apparent cytotoxicity. Both phenazine derivatives inhibited chlamydial inclusions formation and growth in a dose-dependent manner. They inhibited Chlamydia infection by reducing elementary body infectivity and disturbing Chlamydia growth at the mid-stage of the chlamydial developmental cycle. Conclusion: Our findings suggest C-4 aryl and C-4 amino phenazine derivatives as promising lead molecules for antichlamydials development.
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