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新型吡唑甲酰胺及异恶唑醇吡唑羧酸酯衍生物的合成与抗真菌活性

Synthesis and antifungal activity of the derivatives of novel pyrazole carboxamide and isoxazolol pyrazole carboxylate.

作者信息

Sun Jialong, Zhou Yuanming

机构信息

College of Chemistry and Pharmaceutical Sciences, Qingdao Agricultural University, Qingdao 266109, China.

出版信息

Molecules. 2015 Mar 9;20(3):4383-94. doi: 10.3390/molecules20034383.

Abstract

A series of pyrazole carboxamide and isoxazolol pyrazole carboxylate derivatives were designed and synthesized in this study. The structures of the compounds were elucidated based on spectral data (infrared, proton nuclear magnetic resonance and mass spectroscopy). Then, all of the compounds were bioassayed in vitro against four types of phytopathogenic fungi (Alternaria porri, Marssonina coronaria, Cercospora petroselini and Rhizoctonia solani) using the mycelium growth inhibition method. The results showed that some of the synthesized pyrazole carboxamides displayed notable antifungal activity. The isoxazole pyrazole carboxylate 7ai exhibited significant antifungal activity against R. solani, with an EC50 value of 0.37 μg/mL. Nonetheless, this value was lower than that of the commercial fungicide, carbendazol.

摘要

本研究设计并合成了一系列吡唑甲酰胺和异恶唑醇吡唑羧酸酯衍生物。基于光谱数据(红外光谱、质子核磁共振光谱和质谱)对化合物的结构进行了阐明。然后,使用菌丝体生长抑制法,对所有化合物进行了针对四种植物病原真菌(葱链格孢、苹果盘二孢、芹菜尾孢和立枯丝核菌)的体外生物测定。结果表明,一些合成的吡唑甲酰胺表现出显著的抗真菌活性。异恶唑吡唑羧酸酯7ai对立枯丝核菌表现出显著的抗真菌活性,EC50值为0.37μg/mL。尽管如此,该值低于商业杀菌剂多菌灵的值。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9d3c/6272414/94aa2f6d32b5/molecules-20-04383-g001.jpg

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