天然除草活性化合物研究进展

综述了近年来国内外从天然产物中开发具有除草活性化合物的研究概况,着重介绍一些可能具有除草剂开发潜力的植物和微生物源化合物,并对生物除草剂的发展前景进行了展望.     

诱集植物在农业害虫综合治理中的应用

综述了近年来国内外从天然产物中开发具有除草活性化合物的研究概况,着重介绍一些可能具有除草剂开发潜力的植物和微生物源化合物,并对生物除草剂的发展前景进行了展望.     

生物除草剂研究与开发的现状及未来的发展趋势

随着公众健康和环保意识的提高以及现代有机农业的快速发展,生物除草剂的开发越来越受到关注。目前全球正式登记或者商业化的生物除草剂产品已经有20多个,其中也不乏国际化产品。然而,由于生物除草自身的局限性,严重限制了这些产品在国际上的市场规模。本文从生物除草剂发展背景和迫切性开始,总结了生物除草剂的类型、全球生物除草剂的研发现状和未来的发展方向。重点分析了以天然活性产物为库源,开发新的生物源除草剂或以天然产物为前体合成新的化学除草剂的可行性、已有的成绩和未来的发展前景。     

植物甲醇提取物的除草活性测定方法研究

本研究通过对植物材料除草活性测定方法的研究,探索在除草活性测定过程中引起误差的几个因素及可能引起误差的几个原因,为今后植物源除草剂的开发提供测定方法。     

具有除草活性植物病原真菌毒素的作用模式

作用模式得到明确的具有除草活性的植物病原真菌毒素为数不多,主要是危害农作物的病原真菌产生的植物毒素,目前只有少数几个具有除草活性的杂草病原真菌植物毒素的作用模式得到鉴定。而近些年来,新获得的绝大多数具有除草活性的杂草病原真菌植物毒素的作用模式尚未得到鉴定。在作用模式已经明确的具有除草活性的植物病原真菌毒素中,除了极个别与有些化学合成除草剂共享相同作用模式,绝大多数具有与现有化学合成除草剂完全不同的作用模式和独特的分子靶标位点,很有希望开发成为新型除草剂。本文重点介绍了目前已经得到鉴定的具有除草活性的植物病原真菌毒素的作用模式。     

天然产物除草剂研究进展

本文综述了天然产物除草剂即生物源除草剂的基本概念、特点、分类和研究进展,概括了天然产物除草剂面临的问题及发展方向。主要介绍了植物源除草剂和微生物源除草剂的研究概况,为应用天然产物进行杂草防除提供理论依据,促进天然产物除草剂的研究。     

含咪唑啉酮结构的吡唑类对羟基苯基丙酮酸双加氧酶抑制剂的除草活性及选择性研究

对羟基苯基丙酮酸双加氧酶（HPPD）是一种重要的除草剂作用靶标。为了发现具有高活性和高选择性的新型HPPD抑制型除草剂,对前期合成的23个含咪唑啉酮结构单元的吡唑类衍生物（2A~2W）进行了深入的生物活性评价和构效关系研究,比较了它们对拟南芥HPPD（AtHPPD）和人源HPPD（hHPPD）抑制活性的差异,从酶水平上总结了该类化合物的结构-活性关系和种属选择性规律,从活体植株水平研究了它们的除草活性。结果表明:部分化合物表现出良好的除草活性和作物安全性,其中化合物2E和2G在150 g/hm2剂量下对荠菜、繁缕、小藜和棒头草抑制活性达到80%以上,且其对作物的安全性也明显优于商品化除草剂硝磺草酮。此外,化合物2P在酶水平上的选择性倍数高达93倍,展示出良好的应用潜力。     

磺酰脲类除草剂与杂草对其抗性的研究进展

1磺酰脲类除草剂的概况1.1磺酰脲类除草剂的发展20世纪70年代末,美国杜邦公司Levitt等首次开发和报道了磺酰脲类除草剂绿磺隆的除草活性[1]。80年代初,这一除草剂开始进行大规模商品化生产,此后,又不断研制和开发了许多磺酰脲类除草剂新品种。此类除草剂问世以后,以其活性高、选择性强、杀草谱广及对动物安全等特性在世界各地得到广泛应用。目前有关磺酰脲类除草剂的专利有400多项,已商品化的有30多种。这类除草剂有很高的除草效率,用量一般为2~100 g/hm2,比传统除草剂的除草效率高100~1 000倍[2]。磺酰脲类除草剂对动物低毒,在非靶标生物…     

植物源抗真菌活性物质研究进展

本文综述了2005-2009年发现的对植物病原真菌具有抑制活性的化合物,并对这些植物源抗真菌活性物质的分布及结构特点进行了简要分析,其中着重介绍了菊科和伞形科植物中的抗真菌活性物质,并对植物源抗真菌活性物质的筛选及开发提出了一些看法和建议。     

葱紫斑病菌毒素的纯化及除草活性

随着人们对植物病原真菌毒素研究和认识的深入,毒素在农药研究中的应用也日趋广泛,特别是把植物病原真菌毒素作为开发除草剂的内源活性物质已有成功的实例。Suemitsu等报道葱紫斑病菌(Alternaria porri)毒素(以下简称AP-毒素)由4种物质组成,但有关其除草生物活性研究目前尚未见报道。作者对AP-毒素的分离提纯及对稗草的生物活性作了初步研究,结果如下。 1 材料与方法 1.1 供试材料:菌种:葱紫斑病菌(Alternaria porri)是由典型病斑分离获得的纯培养物。     

茎叶处理型除草剂使用中应注意的问题

本文从喷雾器械、药液的理化性能和除草剂的组合使用方面概述了茎叶处理型除草剂使用中应该注意的问题。     

类胡萝卜素生物合成抑制剂研究进展

概述了类胡萝卜素生物合成抑制剂类除草剂的作用机理以及八氢番茄红素去饱和酶(phytoene desaturase, PD酶)抑制剂的结构-活性关系。简要介绍了进入商品化开发应用的类胡萝卜素生物合成抑制剂类除草剂品种以及它们的除草活性。     

Synthesis and herbicidal potential of substituted aurones

BACKGROUND: With the objective of exploring the herbicidal activity of substituted aurones, a series of 4,6‐disubstituted and 4,5,6‐trisubstituted aurones were synthesised, and their herbicidal activities against Brassica campestris L. and Echinochloa crusgalli (L.) Beauv. were evaluated in laboratory bioassays. Effects of some of the compounds were evaluated on seed germination. The most active compounds in the laboratory were evaluated in the greenhouse. RESULTS: The compounds were characterised by ¹H NMR, ¹³C NMR and HRMS; some of them were further identified by IR. A (Z)‐configuration was assigned to the aurones, based on spectroscopic and crystallographic data. Bioassay results of root growth showed that the aurones had a moderate herbicidal activity against the dicotyledonous plant Brassica campestris. (Z)‐2‐Phenylmethylene‐4,6‐dimethoxy‐3(2H)‐benzofuranone(6o) was the most active compound, with 81.3 and 88.5% inhibition at 10 and 100 µg ml^?1 respectively, equal to the activity of mesotrione. Some of the aurones possessed some inhibition of germination on several plant species. For glasshouse tests, the substituted aurones had lower herbicidal activity than metolachlor and mesotrione. CONCLUSION: It is possible that aurone derivatives, which possess structures different from those of the commercial herbicides, may become novel lead compounds for the development of herbicides against dicotyledonous weeds with further structure modification. Copyright © 2012 Society of Chemical Industry     

An evaluation of the herbicidal and plant growth regulatory activity of a novel class of carbohydrate-derived 6,8-dioxabicyclo[3.2.1]octanes

Thirty-five carbohydrate-derived dioxabicyclo[3.2.l]octane derivatives have been tested for herbicidal and plant growth regulatory (PGR) activity in an Arabidopsis thaliana assay. Nine of these were herbicidal at concentrations of ? 16 μg ml^?1 in the growth medium. Three compounds, viz, 1,6-anhydro-3-deoxy-4-O-(2,6-dichlorobenzyl)-2-O-methyl-β-D-ribo-hexopyranose(I), its 4-O-benzyl analogue (II), and l,6-anhydro-2-azido-4-O-benzyl-2,3-dideoxy-β-D-ribo-hexopyranose (III) were very active herbicides, killing plants by the rosette stage at 1 μg ml^?1 or less. At lower rates, the herbicides acted as growth regulators, reducing growth rates of shoots and roots as well as flowering and seed-pod development. A further 14 compounds exerted PGR effects only, while 12 compounds were virtually inactive at 16 μg ml^?1, the highest rate tested. The ability of the active compounds to reduce seed viability on mature plants at sublethal concentrations was demonstrated in four cases.     

Pyrimidinyl-substituted amides and thioureas: syntheses, crystal structure and herbicidal activities

BACKGROUND: The high herbicidal activities of [1,2,4]triazolo[1,5-c]pyrimidine and 2H-1,2,4-thiadiazolo[2,3-a]pyrimidine derivatives suggested the development of new fused heterocyclic compounds for application as herbicides. RESULTS: Three series of pyrimidinyl-substituted thioureas (4) and amides (5, 6) were synthesized, and the typical crystal structure of a 2H-1,2,4-thiadiazolo[2,3-a]pyrimidine derivative (5a) was determined by X-ray diffraction. All the compounds were tested for herbicidal activity against selected weeds. CONCLUSION: The series of fused heterocyclic amides 5a to 5d exhibited high herbicidal activities both against monocotyledonous weeds (Echinochloa crus-galli L., Sorghum bicolor (L.) M?nch., Digitaria sanguinalis (L.) Scop) and against dicotyledonous weeds (Amaranthus retroflexus L. and Brassica campestris L.) in pre-emergence treatments. In particular, compound 5b at low concentration still showed high inhibitory activity against A. retroflexus in pre-emergence treatment. Different substituents at the meta positions of the pyrimidine ring were found to affect the herbicidal activity.     

HERBICIDES AS FERTILIZER ADDITIVES

Summary. Granulated compound fertilizers were tested as solid carriers for a variety of herbicides known to be active when applied as liquids.
Pasture and cereal experiments with 2,4-D and MCPA as fertilizer additives indicated considerable loss of herbicidal activity in comparison with spray formulations.
Residual herbicides such as TCA, propham and diuron retained their activity when added to fertilizer for application to root crops. The most effective of the herbicides used as fertilizer additives were TCA and propham, both of which gave good control of Avena fatua in sugar beet, and a mixture of chlorpropham and diuron gave promising results as a general weed control treatment in carrots.
It is concluded that the addition of these or similar herbicides to fertilizer granules may have advantages over conventional spray formulations for those crops which require broadcast pre-sowing applications of herbicides and fertilizer. For such crops the use of a granular fertilizer as the carrier instead of inert material could also have advantages over conventional granular herbicides, particularly by reducing transport and application costs.     

The herbicidal activity of 2-alkyl-2-cyanoacetanilides

The pre-emergent herbicidal activity of 2-alkyl-2-cyanoacetanilide derivatives (a new class of anilide herbicides) is reported and the relationship between structure and activity examined. The compounds appear to act by inhibiting development of root growth. Comparisons with 2-chloroacetanilide herbicides reveal similarities and differences which suggest that, whilst both groups may interact at a similar cellular site, a different reaction mechanism may be involved.     

Phytotoxicants from microorganisms and related compounds

Phytotoxic compounds produced by microorganisms are reviewed. Their utilisation as leads to new herbicides is explored in three chemical classes : 2-aminoalk-3-enoic acids, ether derivatives of 3-hydroxycyclobut-3-ene-1,2-diones, and 2-(acylaminooxy)acetic acid derivatives. It is concluded that some bacteria and fungi yield compounds possessing sufficient herbicidal activity to be valuable as herbicides as such, or as leads for chemical optimisation.     

Aryl chain analogues of the biotin vitamers as potential herbicides. Part 3

Novel aryl chain isosters and analogues of 7-keto-8-aminopelargonic acid (KAPA) and 7,8-diaminopelargonic acid (DAPA), the vitamer intermediates involved in the biosynthetic pathway of biotin, possessing chain lengths of eight carbon atoms, were prepared and evaluated as potential herbicides. In the greenhouse test the most active compounds were the fluorinated derivative 9d and the selenophenyl/furan mixture 17m/17p, which were most active against Foxtail millet. In the more sensitive Arabidopsis test the most active substances were 9a and 17m, which displayed GR(50) (concentration of active compound causing 50% growth inhibition) values of 0.2 and 0.5 mg kg(-1) respectively (values of < 50 mg kg(-1) are considered herbicidal).     

吡啶衍生物研究(IX):N-(1-甲氧羰基)乙基-N-[5-(2-氯吡啶-4-基)-1,3,4-噻二唑-2-基]酰胺的合成及除草活性

为了进一步研究前期发现的除草先导化合物2-仲丁氨基-5-(2-氯吡啶-4-基)-1，3，4-噻二唑(BCPT)的结构-活性关系并提高其除草活性，设计并合成了一系列N-(1-甲氧羰基)乙基-N-[5-(2-氯吡啶-4-基)-1，3，4-噻二唑-2-基]酰胺类化合物。其苗后除草活性测定结果表明，所有化合物的活性都远低于BCPT本身。说明BCPT可能具有与传统酰胺类除草剂不同的作用机制。