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Thiazolino 2-Pyridone Amide Isosteres As Inhibitors of Chlamydia trachomatis Infectivity
Journal of Medicinal Chemistry ( IF 7.3 ) Pub Date : 2017-11-03 00:00:00 , DOI: 10.1021/acs.jmedchem.7b00716
James A. D. Good 1, 2 , Martina Kulén 1, 2 , Jim Silver 2, 3, 4 , K. Syam Krishnan 1, 2 , Wael Bahnan 2, 3, 4 , Carlos Núñez-Otero 2, 4, 5 , Ingela Nilsson 2, 3, 4 , Emma Wede 2, 3, 4 , Esmee de Groot 2, 3, 4 , Åsa Gylfe 2, 4, 5 , Sven Bergström 2, 3, 4 , Fredrik Almqvist 1, 2
Affiliation  

Chlamydia trachomatis is a global health burden due to its prevalence as a sexually transmitted disease and as the causative agent of the eye infection trachoma. We recently discovered 3-amido thiazolino 2-pyridones which attenuated C. trachomatis infectivity without affecting host cell or commensal bacteria viability. We present here the synthesis and evaluation of nonhydrolyzable amide isosteres based on this class, leading to highly potent 1,2,3-triazole based infectivity inhibitors (EC50 ≤ 20 nM).

中文翻译:

噻唑啉酮2-吡啶酮酰胺等排体作为沙眼衣原体感染性的抑制剂

由于沙眼衣原体作为性传播疾病和眼感染沙眼的病原体的流行,沙眼衣原体是全球性的健康负担。我们最近发现了3-酰胺基噻唑啉酮2-吡啶酮,它们可减轻沙眼衣原体的感染力,而不影响宿主细胞或共生细菌的生存能力。我们在这里提出基于此类非水解酰胺等排物的合成和评价,从而导致高度有效的1,2,3-三唑基于感染性抑制剂(EC 50 ≤20纳米)。
更新日期:2017-11-03
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