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Synthesis and antifungal activity of imidazo[1,2-b]pyridazine derivatives against phytopathogenic fungi.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-03-26 , DOI: 10.1016/j.bmcl.2020.127139
Lingling Fan 1 , Zhongfu Luo 1 , Yi Li 1 , Xinyun Liu 1 , Judi Fan 1 , Wei Xue 2 , Lei Tang 1 , Yong Li 1
Affiliation  

A series of 3,6-disubstituted imidazo[1,2-b]pyridazine derivatives have been synthesized and characterized with spectroscopic analyses. The antifungal activities of these compounds against nine phytopathogenic fungi were evaluated by the mycelium growth rate method. The in vitro antifungal bioassays indicated that most of compounds displayed excellent and broad-spectrum antifungal activities. Especially, compounds 4a, 4c, 4d, 4l and 4r exhibited 1.9–25.5 fold more potent than the commercially available fungicide hymexazol against Corn Curvalaria Leaf Spot (CL), Alternaria alternate (AA), Pyricularia oryzae (PO) and Alternaria brassicae (AB) strains. Structure-activity relationship analysis showed that the enhanced antifungal activity is significantly affected by the substituents on the benzene ring and pyridazine ring.



中文翻译:

咪唑并[1,2-b]哒嗪衍生物的合成及其对植物病原真菌的抗真菌活性。

已经合成了一系列的3,6-二取代的咪唑并[1,2- b ]哒嗪衍生物,并通过光谱分析对其进行了表征。通过菌丝体生长速率法评估了这些化合物对9种植物病原真菌的抗真菌活性。中体外抗真菌生物测定法表明,大多数化合物都显示出优良的和广谱的抗真菌活性。特别是,化合物4a4c4d4l4r的效价比市售的杀菌剂羟甲唑对玉米弯刀叶斑(CL),交替链格孢菌(AA),稻瘟病菌(PO)和芸苔念珠菌(AB)菌株。结构-活性关系分析表明,增强的抗真菌活性受到苯环和哒嗪环上取代基的显着影响。

更新日期:2020-03-26
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