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目的设计合成2,3,3a,4-四氢硫色烯并[4,3-c]吡唑类化合物,并对其抗真菌活性进行初步评价。方法以取代苯硫酚为起始原料,首先合成中间体3-次苄基硫色满酮;然后利用水合肼和3-次苄基硫色满酮在醋酸中反应生成目标化合物。采用二倍稀释法对目标化合物的体外抗真菌活性进行测试。结果共合成了8个新的2,3,3a,4-四氢硫色烯并[4,3-c]吡唑类化合物,并经过H-核磁共振、质谱和元素分析等确认了其结构。抗真菌活性实验结果表明,目标化合物对大部分供试真菌具有好的活性。结论2,3,3a,4-四氢硫色烯并[4,3-c]吡唑类化合物在体外具有抗真菌活性,有待深入研究。
Objective To design and synthesize 2, 3, 3a, 4-tetrahydrothiochromen [4,3-c] pyrazoles and evaluate their antifungal activities. Methods The substituted thiophenol was used as the starting material to synthesize the intermediate 3-benzylbenzyl thiochromanone. The target compound was synthesized by the reaction of hydrazine hydrate and 3-benzylbenzyl thiochromanone in acetic acid. In vitro antifungal activity of the compounds of interest was tested using a two-fold dilution. Results A total of eight novel 2,3,3a, 4-tetrahydrothiochromen [4,3-c] pyrazoles were synthesized and their structures were confirmed by H-NMR, MS and elemental analysis . Antifungal activity The experimental results show that the target compound has good activity on most of the tested fungi. Conclusion 2,3,3a, 4-tetrahydrothiochromeno [4,3-c] pyrazoles have antifungal activity in vitro and need further study.