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合成一组新的脂肪族酰肼衍生物及其分子结构与生物活性的相关性。

Synthesis of a new group of aliphatic hydrazide derivatives and the correlations between their molecular structure and biological activity.

机构信息

Department of Chemistry, University of Life Sciences in Lublin, ul. Akademicka 15, 20-950 Lublin, Poland.

出版信息

Molecules. 2012 Mar 22;17(3):3560-73. doi: 10.3390/molecules17033560.

Abstract

In view of the growing demand for new compounds showing biological activity against pathogenic microorganisms, such as pathogenic and phytopathogenic fungi, the objective of this study was to synthesize a new group of aliphatic and aromatic derivatives of hydrazide. In consequence of the reactions observed during synthesis, the resulting compounds retained their linear structure. Their structure and lipophilicity, measured by high-performance liquid chromatography (HPLC), were analyzed. Correlations were determined between the compounds' molecular parameters and biological activity against Fusarium solani and Fusarium oxysporum fungi. The investigated compounds were also examined for their antifungal activity against Aspergillus fumigatus. The obtained results indicate that compounds with fluorine-containing substituents penetrate the cell structure more effectively and are characterized by higher antifungal potential than analogues with different substituents.

摘要

鉴于对具有生物活性的新型化合物的需求不断增长,例如针对致病微生物(如致病真菌和植物病原真菌)的化合物。本研究的目的是合成一组新的脂族和芳族酰肼衍生物。在合成过程中观察到的反应的结果,得到的化合物保留了其线性结构。通过高效液相色谱法(HPLC)对其结构和亲脂性进行了分析。确定了化合物的分子参数与对尖孢镰刀菌和腐皮镰刀菌真菌的生物活性之间的相关性。还研究了所研究的化合物对烟曲霉的抗真菌活性。获得的结果表明,含氟取代基的化合物更有效地穿透细胞结构,并且表现出比具有不同取代基的类似物更高的抗真菌潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b741/6268134/cf7cfd695d71/molecules-17-03560-g004.jpg

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