蕈毒碱类抗白粉病药物分子的设计、合成及药物活性筛选

项目名称： 蕈毒碱类抗白粉病药物分子的设计、合成及药物活性筛选

项目编号： No.21462043

项目类型： 地区科学基金项目

立项/批准年度： 2015

项目学科： 环境化学

项目作者： 穆赫塔尔·伊米尔艾山

作者单位： 新疆大学

项目金额： 53万元

中文摘要： 从生物体中寻找高效、低毒且结构新颖的化合物并对其结构进行优化，是新农药创制领域的研究热点之一。以天然产物蘑菇中的活性物质蕈毒碱的结构为模型，采用分子重组法，吖啶、五元杂环、六元杂环与异噁唑为基元结构的蕈毒碱拼接，从分子的立体结构、氢键性、电性和亲水性方面出发，对其进行结构修饰和优化，设计合成系列螺稠杂蕈毒碱类似物，增强异噁唑啉环上的吖啶与细菌细胞DNA 分子的结合力，从而降低药剂的耐药性和毒性，提高其药性，通过实验室盆栽试验测出化合物对白粉病的防效效果，田间试验验证高活性化合物防止白粉病的药效。根据蕈毒碱类似物抗菌活性筛选数据，用SPSS软件最小显著差数法，对病情指数和抑制率进行显著性分析，深入研究化合物的构效关系。在田间抗甜菜白粉病菌药效验证数据，进一步进行结构修饰，预期获得若干具有高效抗白粉病效果的蕈毒碱类化合物，为新型抗白粉病药物的设计合成及新型农药的开发、应用提供一定的理论基础。

中文关键词： 草毒碱类；白粉病；药物分子设计；活性筛选

英文摘要： Looking for high efficiency, low toxicity and new compounds from the organisms and optimizing its structure, is one of the hot field of the new pesticide research, the active substances muscurine in the mushroom as a structure model, applying molecular recombination method, isoxazole muscurine as a primitive structure connect acridine, five-and six-membered heterocycles, starting from molecular spatial structure, hydrogen bonding, electrical resistance and hydrophilic property, Structure modification and optimization for it, synthesis series of muscurine analogues, enhance the isoxazoline ring of acridine adhesion with DNA molecule in bacterial cells, there by reducing the drug-fast and toxicity of the Pharmacy, improve its property. By pot experiment measuring the control effect of powdery mildew on the compounds, field test validated efficiency of highly active compounds against powdery mildew Fungi. According to there antibiosis activity using the SPSS software least significant difference method.conduct field experiment to verify the antibiosis activities on erysiphe cichoracearum on sugarbeet to modify there structure. In-depth studies of the relationships of structure-activity on compounds. In order to design drugs and synthesis of new anti- powdery mildew Fungi and development of new pesticides, provides the theoretical basis on the application.

英文关键词： Muscarine;Powdery Mildew Fungi;durg molecular design;drug screening