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首页> 外文期刊>Journal of Agricultural and Food Chemistry >Late-Stage C-H Functionalization of Nicotinamides for the Expedient Discovery of Novel Antifungal Leads
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Late-Stage C-H Functionalization of Nicotinamides for the Expedient Discovery of Novel Antifungal Leads

机译：Nicotinamides的后期C-H官能化，以实现新型抗真菌铅的权宜之计

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摘要

Encouraged by the successful flexible modifications of the succinate dehydrogenase inhibitors, antifungal activity guided by the divergent synthesis of nicotinamides of the prevalidated pharmacophore 2-(2-oxazolinyl)aniline was conducted. The work highlighted the first utilization of the late-stage C-H functionalization assisted by the innate pharmacophore for the discovery of promising agrochemicals. New synthetic methodology and antifungal exploration of alkoxylated nicotinamides were accomplished. Fifty-five functionalized nicotinamides of 7 types were rationally designed and efficiently prepared through C-H functionalization, which facilitated the acquirement of four N-para aryloxylated nicotinamides (E3, E13, E19, and E22) as potential antifungal candidates against Botrytis cinerea, with the EC50 values lower than 5 mg/L. In vivo/vitro biotest, molecular docking, and structural analysis reconfirmed the novelty and practical potential of the antifungal candidates E3 and E19. This operationally simple platform will provide various "polar parts" and offer intriguing opportunities for the optimization of the carboxamide fungicides and structure-related pharmaceuticals.
机译：通过成功灵活的琥珀酸脱氢酶抑制剂的柔性修饰来鼓励，进行抗真菌酰胺的抗真菌活性的抗真菌酰胺，进行了预防的药物2-（2-恶唑啉基）苯胺的含量。该工作突出了先天药物协助的第一次利用先天药物辅助，用于发现有前途的农用化学品。完成了烷氧基化烟酰胺的新的合成方法和抗真菌探索。通过CH官能化合理设计和有效地制备了505个官能化的烟酰胺，通过CH官能化进行了合理的设计和有效地制备，这促进了与EC50对抗Botrytis Cinerea的潜在抗真菌候选者的四个N-PARARAx化的烟酰胺（E3，E13，E19和E22）。值低于5 mg / L.在体内/体外，分子对接和结构分析重新确认了抗真菌候选者E3和E19的新颖性和实际潜力。该操作简单的平台将提供各种“极性部分”，并为优化羧胺杀菌剂和结构相关药物提供有趣的机会。

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