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含喹唑啉酮部分的杨梅素衍生物的设计、合成、抗菌活性、抗病毒活性及作用机制

Design, Synthesis, Antibacterial Activity, Antiviral Activity, and Mechanism of Myricetin Derivatives Containing a Quinazolinone Moiety.

作者信息

Liu Tingting, Peng Feng, Cao Xiao, Liu Fang, Wang Qifan, Liu Liwei, Xue Wei

机构信息

State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Research and Development Center for Fine Chemicals, Guizhou University, Guiyang 550025, P. R. China.

出版信息

ACS Omega. 2021 Nov 4;6(45):30826-30833. doi: 10.1021/acsomega.1c05256. eCollection 2021 Nov 16.

Abstract

Plant bacteria such as (), (), (), and tobacco mosaic virus (TMV) have created huge obstacles to the global trade of food and economic crops. However, traditional chemical agents used to control these plant diseases have gradually become disadvantageous due to long-term irregular use. Therefore, finding new and efficient antibacterial and antiviral agents is becoming imperative. In this study, a series of myricetin derivatives containing a quinazolinone moiety were designed and synthesized, and the antibacterial and antiviral activities of these compounds were evaluated. The bioassay results showed that some target compounds exhibited good antibacterial activities and antiviral activities . Among them, the median effective concentration (EC) value of compound against was 16.9 μg/mL, which was better than those of the control drugs bismerthiazol (BT) (62.2 μg/mL) and thiodiazole copper (TC) (97.5 μg/mL). Scanning electron microscopy (SEM) results confirmed that compound inhibited the growth of by affecting the morphology of cells. Microscale thermophoresis (MST) test results indicated that the dissociation constant ( ) value of compound against TMV-CP was 0.012 μM, which was better than that of the control agent ningnanmycin (2.726 μM). This study reveals that myricetin derivatives containing a quinazolinone moiety are potential antibacterial and antiviral agents.

摘要

诸如()、()、()等植物细菌以及烟草花叶病毒(TMV)给全球粮食和经济作物贸易造成了巨大障碍。然而,由于长期不规范使用,用于防治这些植物病害的传统化学药剂已逐渐显现出弊端。因此,寻找新型高效的抗菌和抗病毒药剂变得势在必行。在本研究中,设计并合成了一系列含有喹唑啉酮部分的杨梅素衍生物,并对这些化合物的抗菌和抗病毒活性进行了评估。生物测定结果表明,一些目标化合物表现出良好的抗菌活性和抗病毒活性。其中,化合物对()的半数有效浓度(EC)值为16.9μg/mL,优于对照药物叶枯唑(BT)(62.2μg/mL)和噻菌铜(TC)(97.5μg/mL)。扫描电子显微镜(SEM)结果证实,化合物通过影响细胞形态抑制了()的生长。微量热泳动(MST)测试结果表明,化合物对TMV-CP的解离常数()值为0.012μM,优于对照药剂宁南霉素(2.726μM)。本研究表明,含有喹唑啉酮部分的杨梅素衍生物是潜在的抗菌和抗病毒药剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d895/8600648/9e28e7c8aa2a/ao1c05256_0002.jpg

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