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Synthesis of Novel Thiazolyl Hydrazine Derivatives and Their Antifungal Activity
Journal of Chemistry ( IF 2.8 ) Pub Date : 2021-08-26 , DOI: 10.1155/2021/6563871
Jianjun Zhu 1 , Yazhen Chen 1 , Fen Su 1 , Peiyi Wang 1
Affiliation  

A series of novel thiazolyl hydrazine derivatives 3a–3o were synthesized and evaluated for their in vitro antifungal activity against six phytopathogenic strains, namely, Botryosphaeria dothidea (B. d.), Gibberella sanbinetti (G. s.), Fusarium oxysporum (F. o.), Thanatephorus cucumeris (T. c.), Sclerotinia sclerotiorum (S. s.), and Verticillium dahliae (V. d.), by the classical mycelial growth rate method. Biological assessment results showed that most of these target compounds showed good antifungal activity toward tested strains. Especially, compound 3l showed excellent antifungal activities against B. d. and G. s. with relatively lower EC50 values of 0.59 and 0.69 µg/mL, respectively, which were extremely superior to those of commercial fungicides fluopyram, boscalid, and hymexazol and were comparable to those of carbendazim. Given the excellent bioactivity of designed compounds, this kind of thiazolyl hydrazine framework can provide a suitable point for exploring highly efficient antifungal agents.

中文翻译:

新型噻唑基肼衍生物的合成及其抗真菌活性

合成了一系列新型噻唑基肼衍生物3a-3o并评估了它们对六种植物致病菌株的体外抗真菌活性,即Botryosphaeria dothidea ( B. d. )、Gibberella sanbinetti ( G. s. )、尖孢镰刀菌( F. o. )、Thanatephorus cucumeris ( T. c. )、Sclerotinia sclerotiorum ( S. s. ) 和Verticillium dahliae ( V. d.),通过经典的菌丝生长率方法。生物学评估结果表明,这些目标化合物中的大多数对受试菌株表现出良好的抗真菌活性。特别是,化合物3lB. d.表现出优异的抗真菌活性G. s. 具有相对较低的 EC 50值,分别为 0.59 和 0.69  µg /mL,这非常优于商业杀菌剂氟吡菌酰胺、啶酰菌胺和毒恶唑,并且与多菌灵相当。鉴于设计的化合物具有优异的生物活性,这种噻唑基肼骨架可以为探索高效抗真菌剂提供合适的点。
更新日期:2021-08-26
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