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追求先导创新:具有药学重要性且独特的无酰胺琥珀酸脱氢酶抑制剂

In Pursuit of Lead Innovation: Pharmaceutically Important and Distinct Amide-Free Succinate Dehydrogenase Inhibitors.

作者信息

Sun Pengzhi, Sun Shengxin, Kong Wenlong, Li Shengkun

机构信息

State Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, China.

出版信息

J Med Chem. 2025 Jan 23;68(2):1051-1067. doi: 10.1021/acs.jmedchem.4c02757. Epub 2025 Jan 1.

Abstract

Though succinate dehydrogenase inhibitors (SDHIs) are quite successful in the modern agrochemical industry, the Fungicide Resistance Action Committee has classified the resistance risk as "medium to high". Structural analysis reveals that these antifungal chemotypes are highly conserved with amides as a consistent feature. This chemical factor may be a potential factor for the ever-increasing resistance risk. Introducing new antifungal structures or models may be a potent method to tackle this and find new bioactive compounds. In this Perspective, the recent progress in SDHIs without amide functionality from either synthetic endeavors or natural sources is showcased, focusing on their biological activities and a brief introduction of their mechanism. Synthetic advances in complex natural products are discussed, aiming to inspire new pharmaceutical discoveries and efficient synthesis methods. The challenges and strategies for the development of SDHIs are also discussed. This may offer insights for developing new SDHIs or chemical entities to combat the increasing resistance to commercial agrochemicals.

摘要

尽管琥珀酸脱氢酶抑制剂(SDHIs)在现代农用化学品行业相当成功,但杀菌剂抗性行动委员会已将其抗性风险归类为“中到高”。结构分析表明,这些抗真菌化学类型高度保守,酰胺是其一致特征。这一化学因素可能是抗性风险不断增加的潜在因素。引入新的抗真菌结构或模型可能是解决这一问题并发现新生物活性化合物的有效方法。在这篇综述中,展示了来自合成努力或天然来源的无酰胺功能的SDHIs的最新进展,重点介绍了它们的生物活性及其作用机制的简要介绍。讨论了复杂天然产物的合成进展,旨在激发新的药物发现和高效合成方法。还讨论了SDHIs开发面临的挑战和策略。这可能为开发新的SDHIs或化学实体以应对对商业农用化学品日益增加的抗性提供见解。

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