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Novel anthranilic amide derivatives bearing the chiral thioether and trifluoromethylpyridine: Synthesis and bioactivity.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2019-12-17 , DOI: 10.1016/j.bmcl.2019.126902 Dexia Luo 1 , Shengxin Guo 1 , Feng He 1 , Heying Wang 2 , Fangzhou Xu 3 , Ali Dai 1 , Renfeng Zhang 1 , Jian Wu 1
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2019-12-17 , DOI: 10.1016/j.bmcl.2019.126902 Dexia Luo 1 , Shengxin Guo 1 , Feng He 1 , Heying Wang 2 , Fangzhou Xu 3 , Ali Dai 1 , Renfeng Zhang 1 , Jian Wu 1
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Ten anthranilic amides bearing skeletons of chiral thioether and trifluoromethylpyridine (5a-5j) were designed and synthesized. Bioassays indicated that some of compounds had excellent insecticidal activity. For example, compounds 5a, 5e and 5g had the median lethal concentrations (LC50) against Plutella xylostella of 7.3, 8.7 and 8.1 µg/mL respectively. The LC50 of 5a against Ostrinia nubilalis and Pseudaletia separata were 21.7 and 44.2 µg/mL respectively. Anti-TMV tests indicated that some compounds also showed good antiviral activity. For instance, the curative activities of compounds 5b and 5e were 57.2% and 63.6%, and with half maximal effective concentration (EC50) of 304.5 and 203.0 µg/mL, respectively, which were much higher than these of ribavirin (39.4%, EC50 = 819.8 µg/mL) and ningnanmycin (56.2%, EC50 = 361.4 µg/mL). The molecular docking between the most active compounds and ryanodine receptor of the Plutella xylostella were also discussed. Those results indicated that the novel anthranilic amide derivatives in present work were worthy of further research and development as novel pesticides.
中文翻译：
带有手性硫醚和三氟甲基吡啶的新型邻氨基苯甲酰胺衍生物：合成和生物活性。
设计并合成了十个带有手性硫醚和三氟甲基吡啶（5a-5j）骨架的邻氨基苯甲酰胺。生物测定表明某些化合物具有优异的杀虫活性。例如，化合物5a，5e和5g相对于小菜蛾的中位致死浓度（LC50）分别为7.3、8.7和8.1 µg / mL。5a的抗念珠菌和分离的假单胞菌的LC50分别为21.7和44.2 µg / mL。抗TMV试验表明，某些化合物还显示出良好的抗病毒活性。例如，化合物5b和5e的治愈活性分别为57.2％和63.6％，最大有效浓度（EC50）的一半分别为304.5和203.0 µg / mL，远高于利巴韦林（39.4％，EC50）。 = 819.8 µg / mL）和宁南霉素（56.2％，EC50 = 361.4 µg / mL）。还讨论了小菜蛾活性最强的化合物与ryanodine受体之间的分子对接。这些结果表明，目前的新型邻氨基苯甲酰胺衍生物作为新型农药值得进一步研究和开发。
更新日期：2019-12-18
中文翻译：
带有手性硫醚和三氟甲基吡啶的新型邻氨基苯甲酰胺衍生物：合成和生物活性。
设计并合成了十个带有手性硫醚和三氟甲基吡啶（5a-5j）骨架的邻氨基苯甲酰胺。生物测定表明某些化合物具有优异的杀虫活性。例如，化合物5a，5e和5g相对于小菜蛾的中位致死浓度（LC50）分别为7.3、8.7和8.1 µg / mL。5a的抗念珠菌和分离的假单胞菌的LC50分别为21.7和44.2 µg / mL。抗TMV试验表明，某些化合物还显示出良好的抗病毒活性。例如，化合物5b和5e的治愈活性分别为57.2％和63.6％，最大有效浓度（EC50）的一半分别为304.5和203.0 µg / mL，远高于利巴韦林（39.4％，EC50）。 = 819.8 µg / mL）和宁南霉素（56.2％，EC50 = 361.4 µg / mL）。还讨论了小菜蛾活性最强的化合物与ryanodine受体之间的分子对接。这些结果表明，目前的新型邻氨基苯甲酰胺衍生物作为新型农药值得进一步研究和开发。
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