Design, Synthesis, and Bioactivity of Novel Quinazolinone Scaffolds Containing Pyrazole Carbamide Derivatives as Antifungal Agents
文献类型： 外文期刊
作者： Lei, Zhiwei 1 ; Yao, Jianmei 2 ; Liu, Huifang 2 ; Bai, Xianjin 3 ; Gao, Xingsi 3 ; Pan, Qiuyuan 3 ; Yang, Wen 2 ;
作者机构： 1.Guizhou Univ, Key Lab Green Pesticide & Agr Bioengn, Minist Educ, Guiyang 550025, Peoples R China
2.Guizhou Acad Agr Sci, Tea Res Inst, Guiyang 550006, Peoples R China
3.Guizhou Educ Univ, Sch Biol Sci, Guiyang 550000, Peoples R China
关键词： fungicidal activity; quinazolinone; pyrazolecarbamide; structure-activity relationship
期刊名称：CURRENT ISSUES IN MOLECULAR BIOLOGY （ 影响因子：2.976； 五年影响因子：3.139 ）
ISSN： 1467-3037
年卷期： 2022 年 44 卷 11 期
页码：
收录情况： SCI
摘要： In this study, 32 novel quinazolinone-scaffold-containing pyrazole carbamide derivatives were designed and synthesized in a search for a novel fungicide against Rhizoctonia solani. Single-crystal X-ray diffraction of 3-(difluoromethyl)-N-(2-((6,7-difluoro-4-oxoquinazolin-3(4H)-yl)methyl)phenyl)-1-methyl-1H-pyrazole-4-carboxamide (6a(11)) confirmed the structure of the target compounds. The in vitro antifungal activity of the target compounds against R. solani was evaluated at 100 mu g/mL. The structure-activity relationship analysis results revealed that antifungal activity was highest when the substitution activity was at position 6. Moreover, the position and number of chlorine atoms directly affected the antifungal activity. Further in vitro bioassays revealed that 6a(16) (EC50 = 9.06 mg/L) had excellent antifungal activity against R. solani that was higher than that of the commercial fungicide fluconazole (EC50 = 12.29 mg/L) but lower than that of bixafen (EC50 = 0.34 mg/L). Scanning electron microscopy), 7.33 (SEM) revealed that N-(2-((6,8-dichloro-4-oxoquinazolin-3(4H)-yl)methyl)phenyl)-3-(difluoromethyl)-1-methyl-1H-pyrazole-4-carboxamide (6a(16)) also affected the mycelial morphology. The findings revealed that molecular hybridization was an effective tool for designing antifungal candidates. Meanwhile, pyrazolecarbamide derivatives bearing a quinazolinone fragment exhibited potential antifungal activity against R. solani.
- 相关文献
作者其他论文 更多>>
-
An ethylvanillin electrocatalytic sensor based on perovskite La 3+-doped barium stannate nanorods
作者：Du, Haijun;Hu, Minkang;Li, Shengnan;Duan, Yu;Wang, Dexiang;Feng, Jun;Du, Haijun;Yang, Wen
关键词：La3+-dopedBaSnO3; Ethylvanillin; Electrocatalytic sensor
-
Plant-derived citronellol can significantly disrupt cell wall integrity maintenance of Colletotrichum camelliae
作者：Zhang, Jiying;Liu, Huifang;Li, Rongyu;Zhang, Jiying;Liu, Huifang;Li, Rongyu;Liu, Huifang;Yao, Jianmei;Ma, Chiyu;Yang, Wen;Lei, Zhiwei;Li, Rongyu
关键词：Colletotrichum camelliae; Tea anthracnose disease; Citronellol; Antifungal activity; Biochemical mechanism
-
Geraniol: A Potential Defense-Related Volatile in "Baiye No. 1" Induced by Colletotrichum camelliae
作者：Chen, Wei;Cheng, Yongjia;Liu, Huifang;Chen, Yao;Ma, Chiyu;Yang, Wen;Liu, Yaoguo
关键词：plant volatiles; Colletotrichum camelliae; geraniol
-
Controlled-Release of Plant Volatiles: New Composite Materials of Porous Carbon-Citral and Their Fungicidal Activity against Exobasidium vexans
作者：Liu, Yaoguo;Chen, Wei;Yin, Jie;Chen, Yao;Liu, Huifang;Lei, Zhiwei;Ma, Chiyu;Yang, Wen
关键词：Exobasidium vexans; porous carbon; citral; controlled release; fungicidal activity
-
Synthesis and Bioactivity of Novel Sulfonate Scaffold-Containing Pyrazolecarbamide Derivatives as Antifungal and Antiviral Agents
作者：Lei, Zhi-Wei;Lei, Zhi-Wei;Yao, Jianmei;Liu, Huifang;Ma, Chiyu;Yang, Wen
关键词：pyrazolecarbamide; sulfonate; antifungal activity; antiviral activity; synthesis
-
A Review on the Extraction, Bioactivity, and Application of Tea Polysaccharides
作者：Yao, Jianmei;Liu, Huifang;Ma, Chiyu;Pu, Lulu;Yang, Wen;Lei, Zhiwei
关键词：Tea Polysaccharides; extraction; bioactivity; antioxidant activity
-
Vectorizing Pro-Insecticide: Influence of Linker Length on Insecticidal Activity and Phloem Mobility of New Tralopyril Derivatives
作者：Li, Tian Xing;Chen, Yao;Liu, Hui Fang;Ma, Chi Yu;Yang, Wen
关键词：insecticide conjugate; glutamic acid; tralopyril; chlorfenapyr; phloem mobility
