细菌病原体需要保守的膜组氨酸传感器激酶（QseC）来检测宿主来源的肾上腺素能信号和细菌自身诱导物3（AI-3），从而激活诱导毒力基因表达的信号级联反应。LED209是一种有效的QseC抑制剂，在体外5 pM时可阻断去甲肾上腺素和肾上腺素触发的QseC依赖性毒力基因的表达。虽然LED209抑制肠出血性大肠杆菌，鼠伤寒沙门氏菌和土拉弗朗西斯菌的毒力，但它不抑制病原体的生长，这是抗菌剂防止药物耐药性的高度理想的功能。 Bacterial pathogens require the conserved membrane histidine sensor kinase (QseC) to detect both host-derived adrenergic signals and the bacterial autoinducer-3 (AI-3), thus activating a signaling cascade that induces virulence gene expression. LED209 is a potent QseC inhibitor that blocks both norepinephrine- and epinephrine-triggered QseC-dependent virulence gene expression at 5 pM in vitro. While LED209 inhibits virulence of enterohemorrhagic E. coli, S. typhimurium, and F. tularensis, it does not inhibit pathogen growth, a highly desirable feature of antimicrobial agents to prevent drug resistance.
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LED209
CAS number：245342-14-7 molecular formula：C19H17N3O2S2
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| Chinese alias | - | ||
| English alias | LED-209;LED 209 | AC-35928 | SCHEMBL3396831 | C74263 | Benzenesulphonamide, N-phenyl-4-(((phenylamino)thioxomethyl)amino)- | FT-0717959 | BS-16236 | 1-phenyl-3-[4-(phenylsulfamoyl)phenyl]thiourea | 1-Phenyl-3-(4-(phenylsulfamoyl)phenyl)thiourea | LED209 | | ||
| CAS number | 245342-14-7 | molecular formula | C19H17N3O2S2 |
| molecular weight | 383.49 g/mol | Exact mass | - |
| PSA | 111.000 Ų | logp | 3.700 |
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