Wang Qiuxiao, Wang Tao, Zhou Yifei, Gao Haixiang
Innovation Center of Pesticide Research, Department of Applied Chemistry, China Agricultural University, Beijing, China.
Pest Manag Sci. 2023 Jan;79(1):114-124. doi: 10.1002/ps.7179. Epub 2022 Oct 19.
As an effective strategy to improve the basic properties of drugs, salt formation was less used in the field of pesticides than the medicine field. It is worth trying to improve the inherent shortcomings of cyprodinil (high K values; polymorphism) in this way to enhance its practicality.
Eight cyprodinil salts (CYP-Salts) were prepared. The properties of CYP-Salts, including solubility in various solvents, polymorphic behavior, soil absorption, photolysis in aquatic water, in vitro fungicidal activity and curative activity, were assessed. It was observed that compared with those of cyprodinil, CYP-Salts had lower soil adsorption, while also having lower log K values and could be more easily photodegraded in water. That is, CYP-Salts have lower impacts on water bodies and aquatic organisms than cyprodinil. Three CYP-Salts showed higher in vitro antifungal activities and curative activity. CYP-Salts have enhanced practicality, as they could avoid possible agglomeration caused by recrystallization.
Salt forming enhanced the properties of Cyprodinil in many aspects. CYP-Salts may potentially become a better substitute for cyprodinil. This study offers a more economical and effective strategy to prepare better alternatives to existing fungicides. © 2022 Society of Chemical Industry.
作为改善药物基本性质的有效策略，盐形成在农药领域的应用比医药领域少。值得尝试通过这种方式改善嘧菌环胺（高K值；多晶型现象）的固有缺点，以提高其实用性。
制备了八种嘧菌环胺盐（CYP盐）。评估了CYP盐的性质，包括在各种溶剂中的溶解度、多晶型行为、土壤吸附、在水中的光解、体外杀菌活性和治疗活性。观察到，与嘧菌环胺相比，CYP盐的土壤吸附较低，同时log K值也较低，并且在水中更容易光降解。也就是说，CYP盐对水体和水生生物的影响比嘧菌环胺小。三种CYP盐表现出更高的体外抗真菌活性和治疗活性。CYP盐具有更高的实用性，因为它们可以避免重结晶引起的可能团聚。
盐形成在许多方面增强了嘧菌环胺的性质。CYP盐可能成为嘧菌环胺更好的替代品。本研究提供了一种更经济有效的策略，以制备现有杀菌剂的更好替代品。© 2022化学工业协会。
