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以芳氧吡啶乙酮分子插件为基础,设计合成了一系列芳氧吡啶乙酮肟醚类化合物,其结构经核磁共振氢谱、碳谱及高分辨质谱等确证。初步杀虫活性测定结果表明,该系列化合物对棉蚜 Aphis gossypii (Glover) 具有较好的杀虫活性,其中化合物 5a 和 6i 在50 μg/mL下对棉蚜的致死率分别为76.8%和70.1%,具有作为先导化合物进一步研究的价值;但其对小菜蛾的杀虫活性较差,在100 μg/mL下的致死率普遍低于30%。该系列化合物主要体现出了新烟碱类化合物的活性特征,为进一步研究其构效关系提供了新思路。 相似文献
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分子模拟在农药半抗原设计及其免疫识别机制中的应用 总被引：1，自引：0，他引：1
免疫半抗原的分子设计与合成是建立小分子免疫化学分析方法的关键步骤。在介绍农药半抗原设计一般策略的基础上,指出分子模拟技术在农药半抗原合理设计中的适用性在于其能通过对分子结构和动力学行为的模拟,获得能表示和解释农药分子免疫原性和生物活性的参数。重点阐述了分子模拟在免疫原和竞争原设计中的应用,揭示了采用分子模拟技术进行半抗原设计的优势在于其能够克服目前半抗原设计方法的经验性和主观随意性。运用分子模拟技术能够更好地研究抗原抗体反应中的分子间作用力,因此该技术有利于促进抗原抗体反应识别机制研究的深入进行。分子模拟技术还能够应用于解释抗体的交叉反应率,从而能应用于提高抗体宽谱性研究。 相似文献
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分子印迹传感技术在农药残留检测中的应用研究进展 总被引：1，自引：1，他引：0
传统的大型仪器检测及免疫检测等农药残留检测方法存在周期长、成本高、操作复杂等局限性。近年来随着分子印迹技术和微电子技术的发展,分子印迹传感技术作为一种新的农药残留检测方法,因其具有快速、实时、操作简便、灵敏度高及特异性好等优点,目前已被应用于多数种类杀虫剂及部分除草剂和植物生长调节剂的残留检测,显示出了广阔的发展前景。文章从原理和方法方面综述了分子印迹传感技术与电化学、光学以及质量敏感技术联用在农药残留检测领域的研究应用进展,并对该技术的未来发展趋势和应用前景进行了展望。 相似文献
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新型杀菌剂的创制在农业可持续发展和克服抗药性中具有重要作用。由于杀菌剂作用机制或靶标是新杀菌剂分子设计合成和创制开发的重要基础,因此作用机制或靶标研究的滞后会阻碍新先导化合物的发现或新品种的创制。鉴于此,本文对目前杀菌剂作用靶标的识别及靶向杀菌剂的分子设计进行了概述。首先阐述了基于转录组学、蛋白质组学的研究和药物亲和层析技术在靶标识别中的应用;其次概述了多学科交叉的方法在分子靶标验证中的应用;最后以strobilurin A为先导的Qo位点抑制剂、以肉桂酸为先导的卵菌抑制剂、以萎锈灵为先导的琥珀酸脱氢酶和植物免疫激活剂等不同类型的靶向杀菌剂为例进行了举例说明。 相似文献
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本书在系统总结作者研究团队长期从事新农药创制研究实践与成果的基础上,紧紧围绕首创的新农药创新研究方法--中间体衍生化法,详细阐述了其在我国新农药创制中的内涵、意义及其应用,具体介绍了包括替换法、衍生法及直接合成法在新农药创制中应用实例,具有极高的学术价值与极强的理论指导意义。本书内容是"中间体衍生化法"与我国新农药创制紧密结合的结晶,所体现的科研成果被应用于实践,取得了重大的经济效益与社会效益,具有很高的学术性、原创性和引领性,将为我国新农药创制提供极强的理论与方法指导。 相似文献
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导向农药是指可在植物体内向特定部位定向传导的农药。通过改善外源物质的传导性 (尤其是韧皮部传导性) 可显著提高导向农药在植物体内的系统性分布,有利于实现精准防控。文章综述了导向农药的分子设计理念、糖基导向农药和氨基酸导向农药的韧皮部传导性及生物活性等方面的研究进展,指出农药分子与相关氨基酸转运蛋白载体之间的构效关系将是今后导向农药研究的重点,同时提出可以激发子作为导向基团,研究开发既能在植物体内通过韧皮部传导防治病虫害,又能激活寄主防御反应、具有植物激活剂性质的新型导向农药的思路。 相似文献
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由稻瘟菌侵染引起的稻瘟病是威胁水稻安全生产最严重的真菌病害之一。鉴定克隆水稻抗稻瘟病基因, 系统深入研究稻瘟菌与水稻的相互作用, 揭示水稻的抗病机制, 进而创制推广抗稻瘟病新材料, 对确保粮食安全具有重要意义。本文总结了近10年来稻瘟病抗病基因和感病基因的鉴定、分子机理解析和应用等进展, 总结归纳了抗病基因聚合、分子设计育种、感病基因编辑、抗病基因的病原诱导表达等抗病育种主要策略。最后提出充分利用种质资源, 利用新技术挖掘新基因及创制新材料, 深入研究叶瘟和穗瘟抗病机制差异等是稻瘟病抗病育种下一步重点研究方向和新挑战。 相似文献
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Yu Zhang Beth A Lorsbach Scott Castetter William T Lambert Jeremy Kister Nick X Wang Carla J R Klittich Joshua Roth Thomas C Sparks Mike R Loso 《Pest management science》2018,74(9):1979-1991
The relentless need for the discovery and development of new agrochemicals continues as a result of driving forces such as loss of existing products through the development of resistance, the necessity for products with more favorable environmental and toxicological profiles, shifting pest spectra, and the changing agricultural needs and practices of the farming community. These new challenges underscore the demand for novel, high‐quality starting points to accelerate the discovery of new agrochemicals that address market challenges. This article discusses the efforts to identify the optimum ranges of physicochemical properties of agrochemicals through analysis of modern commercial products. Specifically, we reviewed literature studies examining physicochemical property effects and analyzed the properties typical of successful fungicides, herbicides, and insecticides (chewing and sap‐feeding pests). From the analysis, a new set of physicochemical property guidelines for each discipline, as well as building block class, are proposed. These new guidelines should significantly aid in the discovery of next‐generation agrochemicals. © 2018 Society of Chemical Industry 相似文献
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Peter Jeschke 《Pest management science》2021,77(1):64-76
To guarantee sustainability and progress, the agrochemical industry is faced with several major challenges. Currently, loss of active ingredients due to consumer perception, changing grower needs and ever‐changing regulatory requirements is far higher than the number being introduced into the market. Therefore, there is a need to develop new products that can provide improved efficacy, selectivity and favorable environmental profiles. Strategies to achieve these goals are the search for acaricides and insecticides with new modes of action, or the discovery of novel molecules with activity on the most attractive target sites having resistance breaking properties against pest species. In this context, the introduction of halogen atoms or asymmetric centers into an active ingredient remains an important tool to modulate their properties, but so too is the pro‐pesticide concept. This review gives an overview of agrochemicals launched over the past 8 years, reflects new insights into known mechanisms of action, and describes the status and outlook for acaricide and insecticide discovery. 相似文献
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Peter Jeschke 《Pest management science》2010,66(1):10-27
The past 30 years have witnessed a period of significant expansion in the use of halogenated compounds in the field of agrochemical research and development. The introduction of halogens into active ingredients has become an important concept in the quest for a modern agrochemical with optimal efficacy, environmental safety, user friendliness and economic viability. Outstanding progress has been made, especially in synthetic methods for particular halogen‐substituted key intermediates that were previously prohibitively expensive. Interestingly, there has been a rise in the number of commercial products containing ‘mixed’ halogens, e.g. one or more fluorine, chlorine, bromine or iodine atoms in addition to one or more further halogen atoms. Extrapolation of the current trend indicates that a definite growth is to be expected in fluorine‐substituted agrochemicals throughout the twenty‐first century. A number of these recently developed agrochemical candidates containing halogen substituents represent novel classes of chemical compounds with new modes of action. However, the complex structure–activity relationships associated with biologically active molecules mean that the introduction of halogens can lead to either an increase or a decrease in the efficacy of a compound, depending on its changed mode of action, physicochemical properties, target interaction or metabolic susceptibility and transformation. In spite of modern design concepts, it is still difficult to predict the sites in a molecule at which halogen substitution will result in optimal desired effects. This review describes comprehensively the successful utilisation of halogens and their unique role in the design of modern agrochemicals, exemplified by various commercial products from Bayer CropScience coming from different agrochemical areas. Copyright © 2009 Society of Chemical Industry 相似文献
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John B. Pillmoor 《Pest management science》1998,52(1):75-80
The work undertaken to isolate the novel, herbicidally active compound, carbocyclic coformycin, to obtain sufficient quantities of the compound for full biological evaluation, and to identify its biochemical mode of action is summarised. Although the compound was extremely active against some weed species, limitations in its spectrum of activity precluded further development. Carbocyclic coformycin exerts its biological action through a novel mode of action by the inhibition of the enzyme adenosine 5′-phosphate deaminase (EC 3.5.4.6) following phosphorylation in planta. From this work, the potential benefits of natural product research in the discovery of new agrochemicals are highlighted along with some of the possible pitfalls. © 1998 SCI. 相似文献
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Peter Jeschke 《Pest management science》2016,72(2):210-225
The synthesis of propesticides is an important concept in design of modern agrochemicals with optimal efficacy, environmental safety, user friendliness and economic variability. Based on increasing knowledge of the biochemistry and genetics of major pest insects, weeds and agricultural pathogens, the search for selectivity has become an ever more important part of pesticide development and can be achieved by appropriate structural modifications of the active ingredient. Propesticides affect the absorption, distribution, metabolism and excretion parameters, which can lead to biological superiority of these modified active ingredients over their non‐derivatised analogues. Various selected commercial propesticides testify to the successful utilisation of this concept in the design of agrochemicals. This review describes comprehensively the successful utilisation of propesticides and their role in syntheses of modern agrochemicals, exemplified by selected commercial products coming from different agrochemical areas. © 2015 Society of Chemical Industry 相似文献
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近红外光谱法快速测定农药中溴氰菊酯含量 总被引：3，自引：0，他引：3
用近红外(NIR)光谱技术结合偏最小二乘法(PLS)进行了敌杀死乳油中有效成分溴氰菊酯含量的快速检测。通过比较敌杀死乳油与常用溶剂的近红外光谱,确定了乳油中使用的溶剂为二甲苯。在敌杀死乳油中加入二甲苯或溴氰菊酯原药来配制不同浓度的校正集,采用PLS建立了有效成分溴氰菊酯的分析模型,模型的决定系数R2、校正标准差(SEC)、交互验证参差均方根(RMSECV)值分别为0.999 9,0.013和0.022。结果表明:近红外光谱技术可以准确测定商品农药制剂中有效成分含量,方法简便、快速,适用于溴氰菊酯制剂的现场、在线分析。 相似文献
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Hanxiang Wu Hanhong Xu Ccile Marivingt‐Mounir Jean‐Louis Bonnemain Jean‐Franois Chollet 《Pest management science》2019,75(6):1507-1516
Systemicity of agrochemicals is an advantageous property for controlling phloem sucking insects, as well as pathogens and pests not accessible to contact products. After the penetration of the cuticle, the plasma membrane constitutes the main barrier to the entry of an agrochemical into the sap flow. The current strategy for developing systemic agrochemicals is to optimize the physicochemical properties of the molecules so that they can cross the plasma membrane by simple diffusion or ion trapping mechanisms. The main problem with current systemic compounds is that they move everywhere within the plant, and this non‐controlled mobility results in the contamination of the plant parts consumed by vertebrates and pollinators. To achieve the site‐targeted distribution of agrochemicals, a carrier‐mediated propesticide strategy is proposed in this review. After conjugating a non‐systemic agrochemical with a nutrient (α‐amino acids or sugars), the resulting conjugate may be actively transported across the plasma membrane by nutrient‐specific carriers. By applying this strategy, non‐systemic active ingredients are expected to be delivered into the target organs of young plants, thus avoiding or minimizing subsequent undesirable redistribution. The development of this innovative strategy presents many challenges, but opens up a wide range of exciting possibilities. © 2018 Society of Chemical Industry 相似文献
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海藻糖是一种非还原性二糖,在昆虫、真菌等有害生物体内参与能量代谢、逆境恢复、几丁质合成等过程。海藻糖酶(EC 3.2.1.28)由于其对海藻糖代谢及其含量调控具有重要作用,且在农业有害生物和哺乳动物体内存在功能差异,已成为开发新型农用化学品的安全型候选靶标。本文对海藻糖酶的晶体结构、海藻糖酶与底物/抑制剂的互作机制研究进展进行了综述;同时对具有农用活性的海藻糖酶抑制剂,如井冈霉素、天然产物salbostatin和trehazolin及其合成类似物、脱氧野尻霉素及其合成类似物、天然生物碱及其合成类似物以及胡椒碱及其类似物的研究进展进行了概述,并重点论述了以胡椒碱为骨架的化合物在农业有害生物防治上的应用。本综述可为靶向海藻糖酶结构进行新型胡椒碱类结构的农用化学品设计与发现提供参考。 相似文献
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本文总结了浙江省近年来农药管理成效,分析了加强农药管理对于服务现代农业发展的重大意义,在此基础上提出了浙江省加快推进现代农药管理的一些对策措施。 相似文献