Department of Applied Chemistry, College of Science, China Agricultural University, Beijing 100193, China.
College of Materials Science and Engineering, Beijing University of Chemical Technology, Beijing 100029, China.
Molecules. 2023 Jun 12;28(12):4722. doi: 10.3390/molecules28124722.
Terbinafine, an inhibitor of squalene epoxidase in ergosterol biosynthesis, is chiefly utilized as an antifungal medication with potential uses in pesticide applications. This study explores the fungicidal efficacy of terbinafine against prevalent plant pathogens and confirms its effectiveness. To augment its water solubility, five ionic salts of terbinafine were synthesized by pairing them with organic acids. Among these salts, TIS 5 delivered the most impressive results, amplifying the water solubility of terbinafine by three orders of magnitude and lessening its surface tension to facilitate better dispersion during spraying. The in vivo experiments on cherry tomatoes showed that TIS 5 had a superior therapeutic activity compared to its parent compound and two commonly used broad-spectrum fungicides, pyraclostrobin and carbendazim. The results highlight the potential of terbinafine and its ionic salts, particularly TIS 5, for use as fungicides in agriculture due to their synergistic effects with furan-2-carboxylate.
特比萘芬是角鲨烯环氧化酶在麦角固醇生物合成中的抑制剂，主要用作抗真菌药物，也有在农药应用中的潜力。本研究探讨了特比萘芬对常见植物病原体的杀菌功效，并证实了其有效性。为提高其水溶性，将特比萘芬与有机酸成盐，合成了 5 种特比萘芬的离子盐。在这些盐中，TIS 5 的效果最为显著，将特比萘芬的水溶性提高了 3 个数量级，并降低了其表面张力，有助于在喷雾时更好地分散。在樱桃番茄上的体内实验表明，TIS 5 的治疗活性优于其母体化合物和两种常用的广谱杀菌剂，吡唑醚菌酯和多菌灵。这些结果表明，特比萘芬及其离子盐，特别是 TIS 5，由于与糠酸的协同作用，具有作为农业用杀菌剂的潜力。
