Design, Synthesis and Biological Evaluation of N-((2-phenyloxazol-4-yl)methyl) Pyrimidine Carboxamide Derivatives as Potential Fungicidal Agents

被引:6
|
作者
Huang, Danling [1 ]
Zheng, Shumin [1 ]
Cheng, Yong-Xian [1 ]
机构
[1] Shenzhen Univ, Sch Pharmaceut Sci, Hlth Sci Ctr, Shenzhen 518060, Peoples R China
关键词
Oxazole derivative; Synthesis; Fungicidal activities; Structure-activity relationship; SULFONYLUREA DERIVATIVES; MEPANIPYRIM; INFECTION;
D O I
10.1515/hc-2020-0117
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Twelve N-((2-phenyloxazol-4-yl)methyl) pyrimidine carboxamide derivatives were designed, synthesized, and characterized by H-1 NMR, C-13 NMR, and HRMS. The fungicidal activities of these new compounds against Sclerotinia sclerotiorum, Botrytis cinereal, and Colletotrichum fragariae were evaluated. The results indicated that compounds 5b, 5f, and 5g displayed potential fungicidal activities against tested fungi, especially 5f exhibited IC50 value of 28.9 mg/L against S. sclerotiorum. Moreover, the compounds 5f and 5g showed IC50 values of 54.8 mg/L and 62.2 mg/L against C. fragariae respectively, which shows that they were more active than the commercial fungicide hymexazol. The superficial structure-activity relationships were discussed, which may be of benefit for the development of fungicides and discovery of novel fungicides.
引用
收藏
页码:185 / 191
页数:7
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