Synthesis and Antifungal Activity of Novel Coumarin Thiazole Derivatives
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Graphical Abstract
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Abstract
In order to find coumarin thiazole derivatives with high antifungal activity, thirteen coumarin thiazole derivatives 8a-8m which have not been reported in literature were synthesized by using 7-hydroxycoumarin as raw material and modifying hydroxyl group. The structures of the products were characterized by ~1H NMR and 13C NMR. The growth rate method was used to determine the antifungal activity of the compound against the pathogenic fungi of sesame: Macrophomina phaseolina, Fusarium oxysporum and Corynespora cassiicola. The results show that all the compounds have certain antifungal activity at the concentration of 500 μg/mL. Among them, the inhibitory activity of N-(4-(3, 4-dichlorophenyl) thiazol-2-yl)-2-(2-oxy-coumarin-7-methoxy) acetamide(8a) is better than dimethomorph against Macrophomina phaseolina, and is equivalent to dimethomorph against Fusarium oxysporum and Corynespora cassiicola. N-(4-(4-thiophen-2-l) thiazol-2-l)-2-(2-oxy-coumarin-7-methoxyxy) acetamide(8k) is close to the control drug in inhibiting the activity of the Macrophomina phaseolina.
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