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

Synthesis and antifungal activity of the derivatives of novel pyrazole carboxamide and isoxazolol pyrazole carboxylate.
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DOI:
10.3390/molecules20034383
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发表时间:
2015-03-09
期刊:
Molecules (Basel, Switzerland)
影响因子:
--
通讯作者:
Zhou Y
Zhou Y
中科院分区:
其他
文献类型:
--
作者:
Sun J;Zhou Y

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本研究设计并合成了一系列吡唑羧酰胺和异恶唑吡唑羧酸酯衍生物。根据光谱数据(红外、质子核磁共振和质谱)对化合物的结构进行了分析。然后采用菌丝体生长抑制法对4种植物病原真菌(黑孢霉、冠状马氏霉、petroselcercospora和solani Rhizoctonia)进行体外生物活性测定。结果表明,部分合成的吡唑类羧酰胺具有明显的抗真菌活性。异恶唑吡唑羧酸酯7ai对茄枯病菌具有显著的抑菌活性,EC50值为0.37 μg/mL。尽管如此,这一数值仍低于商用杀菌剂多菌唑。
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.
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