农药学学报2017，Vol.19Issue(6)：679-687,9.DOI:10.16801/j.issn.1008-7303.2017.0093
齐墩果酸肟醚类化合物的合成及杀菌活性
Synthesis and fungicidal activities of the oleanolic acid oxime ethers
摘要
Abstract
In order to develop potential glucosamine-6-phosphate synthase (GlmS) inhibitors and anti-fungal agents, 30 oleanolic acid oxime ethers were synthesized in an efficient way, and 29 of them were new compounds. The structures of all the synthesized compounds were characterized by1H NMR,13C NMR and HRMS. Preliminary studies based on the Elson-Morgan method and mycelial growth rate method indicated that, many compounds exhibited inhibitory activities against GlmS at the concentration of 0.35 mmol/L. And the inhibition rate of compoundsA-01,A-02,A-04,C-04 andC-05 were about 30%. The original fungicidal activities results showed that some of the compounds exhibited good fungicidal activities toSclerotinia sclerotiorum (Lib.) de Bary,Botrytis cinerea Pers. and Pyricularia oryzae Cav. at the concentration of 50 μg/mL. And the inhibition rate of compoundsA-01, A-02,A-04,A-05 andB-02 againstS. sclerotiorum were about 88%. These compounds will be further studied as potential antifungal lead compounds.关键词
齐墩果酸/肟醚/合成/氨基葡萄糖-6-磷酸合成酶/杀菌活性Key words
oleanolic acid/oxime ether/synthesis/glucoasmine-6-phosphate synthase/fungicidal activity分类
化学化工引用本文复制引用
胡泊洋,赵汗青,陈自力,许晨,赵文婷,赵建庄..齐墩果酸肟醚类化合物的合成及杀菌活性[J].农药学学报,2017,19(6):679-687,9.基金项目
北京市委组织部人才项目(2014000020124g077) （2014000020124g077）
大北农青年教师科研基金(14ZK008) （14ZK008）
高质量论文项目(GJB2015002) （GJB2015002）
北京市教育委员会科技计划一般项目(KM201710020003) （KM201710020003）
高层次创新人才项目(G01040010) （G01040010）
农产品有害微生物及农残安全检测与控制北京市重点实验室开放课题项目.致谢:感谢中国农业大学张建军教授在酶活性研究中提供果糖-6-磷酸及乙酰氨基葡萄糖对硝基苯苷(国家125科技支撑计划No.2015BAK45B01支持研制)试剂的帮助. （国家125科技支撑计划No.2015BAK45B01支持研制）
