Synthesis and Antifungal Activities of Benzophenones

LIN Yan; HUANG Ying-zheng; MA Guang-qiang; CUI Hang-qing; GAO Ying; SHU Ji-cheng

doi:10.13422/j.cnki.syfjx.2017220060

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Synthesis and Antifungal Activities of Benzophenones

更新时间：2024-01-04

- Synthesis and Antifungal Activities of Benzophenones
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 23, Issue 22, Pages: 60-64(2017)
- 作者机构：
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- 基金信息：
- DOI：10.13422/j.cnki.syfjx.2017220060
  CLC： R284;R285
- Published：2017
- 稿件说明：
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LIN Yan, HUANG Ying-zheng, MA Guang-qiang, et al. Synthesis and Antifungal Activities of Benzophenones[J]. Chinese journal of experimental traditional medical formulae, 2017, 23(22): 60-64.
DOI：

LIN Yan, HUANG Ying-zheng, MA Guang-qiang, et al. Synthesis and Antifungal Activities of Benzophenones[J]. Chinese journal of experimental traditional medical formulae, 2017, 23(22): 60-64. DOI： 10.13422/j.cnki.syfjx.2017220060.

摘要

目的：合成二苯甲酮类化合物，对其进行结构表征，并研究其抗真菌活性，初步探讨二苯甲酮类抗真菌活性的构效关系。方法：以苯甲酰氯或邻苯二甲酸酐为原料，经傅克酰基化反应合成二苯甲酮类化合物；经1H-NMR，13 C-NMR和MS-ESI确证结构；通过药敏试验测定目标化合物对4种常见真菌的体外最低抑菌浓度。结果：合成并鉴定出13个二苯甲酮类化合物（a1~a6，b1，c1~c6），均具有不同程度的抗真菌活性（MIC=5.45~1 278 mg ·L-1），其中4-氟-二苯甲酮（a2）抗白色念珠菌活性最强（MIC=55.08 mg ·L-1），4-氯-4'-硝基-二苯甲酮（a4）显示强抗安琪酵母菌活性（MIC=5.45 mg ·L-1），2，4，6-三甲基-二苯甲酮（b1）抗黑曲霉菌活性最好（MIC=55.62 mg ·L-1）。结论：合成的二苯甲酮类化合物具有抗真菌活性，提示二苯甲酮类化合物具有广谱抗真菌性；不同结构对不同真菌具有不同的敏感度，其中羰基官能团对其活性起关键作用，且不同取代基对目标化合物抗真菌活性影响较大，被多个氯原子取代的二苯酮衍生物的抗真菌活性最为突出。实验结果可为二苯甲酮类化合物抗真菌活性的结构修饰提供思路和参考。

Abstract

Objective: To synthesize bezohpenone derivatives

characterize their structures and study their antifungal activities. Method: Benzophenone derivatives were synthesized by Friedel-Crafts acylation reaction with benzoyl chloride or phthalic annhydride as the raw materials. The structures of these compounds were elucidated by 1H-NMR

13C-NMR and MS-ESI. Their effects on minimum inhibitory concentration (MIC) of four fungi were investigated with antimicrobial susceptibility test. Result: The results showed that 13 benzophenone derivatives had antifungal activity in varying degrees

and the carbonyl group was a key to the antifungal activity of benzophenone derivatives. Different substituent groups had significant differences in the effect on their antifungal activities and the diphenyl ketone derivatives with multiple chlorine atoms showed the most excellent antifungal activity. Conclusion: 13 benzophenone derivatives had antifungal activity. The results of this experiment offered a method and reference for structure modification of natural benzophenone compounds with antifungal activity.

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