Thiazolino 2-Pyridone Amide Inhibitors of Chlamydia trachomatis Infectivity
Thiazolino 2-Pyridone Amide Inhibitors of Chlamydia trachomatis Infectivity
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DOI：
10.1021/acs.jmedchem.5b01759
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发表时间：
2016-03-10
影响因子：
7.3
通讯作者：
Almqvist, Fredrik
中科院分区：
文献类型：
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作者：
Good, James A. D.;Silver, Jim;Almqvist, Fredrik
细菌病原体沙眼衣原体是一种全球健康负担，目前采用破坏共生细菌的广谱抗生素进行治疗。我们最近通过表型筛选鉴定了一种化合物，它可以阻断这种细胞内病原体的感染性，且没有宿主细胞毒性（化合物 1，KSK 120）。在此，我们将 1 优化为一类高效的噻唑啉代 2-吡啶酮酰胺 (EC50
The bacterial pathogen Chlamydia trachomatis is a global health burden currently treated with broad-spectrum antibiotics which disrupt commensal bacteria. We recently identified a compound through phenotypic screening that blocked infectivity of this intracellular pathogen without host cell toxicity (compound 1, KSK 120). Herein, we present the optimization of 1 to a class of thiazolino 2-pyridone amides that are highly efficacious (EC50