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硼酸衍生化在农用化学品发现中的潜力及活性

Potential of Boronic Acid Derivatization and Activity in Agrochemical Discovery.

作者信息

Ji Liangshuo, Wu Jianxin, Zuo Yachen, Gao Wenqiang, Feng Jiyao, Zhang Zhenhua

机构信息

College of Science, China Agricultural University, Beijing 100193, China.

College of Plant Protection, China Agricultural University, Beijing 100193, China.

出版信息

Molecules. 2025 Jul 18;30(14):3018. doi: 10.3390/molecules30143018.

DOI:10.3390/molecules30143018
PMID:40733283
Abstract

Since the approval of Bortezomib (Velcade) by the U.S. Food and Drug Administration (FDA) in 2003, boron-containing drugs have successfully entered the global market, spanning therapeutic areas such as anticancer, antibacterial, and antifungal agents. Meanwhile, boron is an essential trace element for plant growth, and boronic acid has been widely used as plant resistance inducers and growth promoters. In 2024, the Fungicide Resistance Action Committee (FRAC) introduced benzoxaboroles as a new category of fungicides, which fully demonstrates the significant application potential of boron-containing compounds (BCCs) in the field of agricultural fungicides. Recently, studies on BCCs in agriculture have emerged continuously. Compared with the systematic reviews in the pharmaceutical field, those focusing on BCCs in agriculture remain absent. This review systematically collates BCCs with reported biological activities from the literature over the past 20 years, from the perspective of boron-containing building blocks. It mainly focuses on the potential of boronic acid derivatization and its activities in agrochemicals. Additionally, it covers the applications of boron-containing building blocks in pharmaceuticals, including their action mechanisms.

摘要

自2003年硼替佐米(万珂)获美国食品药品监督管理局(FDA)批准以来,含硼药物已成功进入全球市场,涵盖抗癌、抗菌和抗真菌剂等治疗领域。同时,硼是植物生长必需的微量元素,硼酸已被广泛用作植物抗性诱导剂和生长促进剂。2024年,杀菌剂抗性行动委员会(FRAC)将苯并氧杂硼唑作为一类新型杀菌剂推出,这充分证明了含硼化合物(BCCs)在农用杀菌剂领域的巨大应用潜力。近年来,农业领域对BCCs的研究不断涌现。与医药领域的系统综述相比,针对农业领域BCCs的综述仍付阙如。本综述从含硼结构单元的角度,系统整理了过去20年文献中报道的具有生物活性的BCCs。它主要关注硼酸衍生化的潜力及其在农用化学品中的活性。此外,还涵盖了含硼结构单元在药物中的应用,包括其作用机制。

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