设计、合成补骨脂素衍生物及其抗真菌活性。
Design, Synthesis and Antifungal Activity of Psoralen Derivatives.
机构信息
Jiangsu Key Laboratory of Pesticide Science, Department of Chemistry, College of Sciences, Nanjing Agricultural University, Nanjing 210095, China.
出版信息
Molecules. 2017 Oct 9;22(10):1672. doi: 10.3390/molecules22101672.
A series of linear furanocoumarins with different substituents have been designed and synthesized. Their structures were confirmed by ¹H-NMR spectroscopy, high resolution mass spectra (EI-MS), IR, and X-ray single-crystal diffraction. All of the target compounds were evaluated in vitro for their antifungal activity against , , , , , and leaf spot at 100 μg/mL, and some of the designed compounds exhibited potential antifungal activities. Compound (67.9%) exhibited higher activity than the control Osthole (66.1%) against . Furthermore, compound (62.4%) represented equivalent antifungal activity as Osthole (69.5%) against . The structure-activity relationship (SAR) study demonstrates that linear furanocoumarin moiety has an important effect on the antifungal activity, promoting the idea of the coumarin ring as a framework that might be exploited in the future.
已经设计和合成了一系列具有不同取代基的线性呋喃香豆素。通过 1H-NMR 光谱、高分辨率质谱（EI-MS）、IR 和 X 射线单晶衍射确认了它们的结构。所有目标化合物都在体外以 100μg/mL 的浓度评估了它们对 、 、 、 、 和 的叶斑的抗真菌活性，一些设计的化合物表现出潜在的抗真菌活性。化合物 （67.9%）对 的活性高于对照奥昔康唑（66.1%）。此外，化合物 （62.4%）对 的抗真菌活性与奥昔康唑（69.5%）相当。构效关系（SAR）研究表明，线性呋喃香豆素部分对抗真菌活性有重要影响，这一发现促进了将香豆素环作为一个可能在未来被利用的框架的想法。
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