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A bird's eye review was tried in Part 2 of this series, 'Phytotoxic sites of action for molecular design of modern herbicides', in order to select the best selection of known and some novel plant-specific targets for molecular design of modern herbicides, which affect amino acid, lipid and cell wall biosynthesis. Although amino acid biosynthesis pathways, particularly those for aromatic amino acids, ammonia assimilation and branched amino acids, have been confirmed as reasonable herbicidal target domains, the other targets affecting plant growth more markedly than inhibition of 5-enolpyruvylshikimate-3-phosphate synthase, glutamine synthetase and acetolactate synthase are discussed. In three essential enzymes involved in fatty acid biosynthesis in or in the vicinity of chloroplasts, acetyl-CoA carboxylase (ACCase), elongase(s) for very long chain fatty acids (VLCFA) and linolate monogalactosyldiacylglycerol desaturase, ACCase and elongase are more important targets for new herbicides. Although the effect of cellulose biosynthesis inhibitors is restricted to cell wall formation in growing plant cells only, there is a good chance to design the low-use rate herbicides also in this class of inhibitors. Other possible targets for new herbicides are also discussed. 相似文献
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Ashkenazi T Pinkert D Nudelman A Widberg A Wexler B Wittenbach V Flint D Nudelman A 《Pest management science》2007,63(10):974-1001
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). 相似文献
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Ashkenazi T Widberg A Nudelman A Wittenbach V Flint D 《Pest management science》2005,61(10):1024-1033
Isosteres 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. The most active compounds, 7-amino-octanoic acid hydrochloride and 7-allyloxy-6-oxo-octanoic acid, displayed Arabidopsis GR50 (concentration of the active compound that causes a 50% growth inhibition) values of 5 and 10 mg kg(-1) respectively. The DAPA analog 6,7-diamino-octanoic acid dihydrochloride, when tested in the greenhouse against six weed species, displayed moderate activity against three species, being most active against foxtail millet. 相似文献
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Studies were conducted to determine the short-term changes in free amino acid levels in the meristematic zone of maize after treatment with various herbicides with different modes of action. These herbicides included inhibitors of various amino acid biosynthetic pathways, photosynthesis, and fatty acids biosynthesis. Inhibitors of various amino acid biosynthetic pathways caused specific reduction in the pools of amino acids being produced by the particular pathway. Inhibitors of other metabolic pathways also caused significant changes in pools of various amino acids. Very similar changes in the pools of amino acids were seen in plants treated with different chemical classes of inhibitors affecting a certain metabolic pathway. However, the changes were quite different between inhibitors of different metabolic processes. The data generated from these studies could be used as a diagnostic tool to determine the mode of action of novel herbicides. 相似文献
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Zlatina Naydenova Gerd-Joachim Krauss Evgeny Golovinsky Konstantin Grancharov 《Pest management science》1999,55(8):825-830
Twelve herbicides, representatives of two chemical groups, substituted phenoxyalkanoic acids and s-triazines, were tested for their inhibitory effect on the glucuronidation of 4-nitrophenol (4-NP), phenolphthalein (PPh) and 4-methylumbelliferone (4-MU) by rat liver microsomes. One millimole MCPA, ametryn and cyanazine significantly decreased PPh UDP-glucuronosyltransferase (UGT) activity, while propazine was found to be a most potent inhibitor of 4-NP glucuronidation. Concentrations of 0.1 mM dichlorprop and cyanazine were still inhibitory against PPh-UGT. The inhibition of 4-MU glucuronidation by the herbicides was low and not specific. As a whole, s-triazine derivatives were more inhibitory than the substituted phenoxyalkanoic acids. Kinetic studies with propazine revealed a non-competitive type of inhibition towards the acceptor substrate 4-NP, with an apparent Ki value of 0.540 mM . With ametryn, an uncompetitive type of inhibition against PPh and a mixed type of inhibition towards UDPGA were found, with apparent Ki values of 0.330 mM and 0.380 mM , respectively. © 1999 Society of Chemical Industry 相似文献
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乙酰乳酸合成酶（AHAS）是支链氨基酸生物合成途径中的一个关键酶,是绿色除草剂的重要作用靶标。由于此生物合成过程只存在于植物和微生物体内,因此该类抑制剂对哺乳动物具有生物安全性。近年来,随着AHAS三维结构的阐明,人们不仅深入了解了已有抑制剂的作用机制,并且依此设计开发了一些新型的抑制剂, 拓展了其在抑菌活性方面的生物学功能。文章对近年来AHAS及其抑制剂的最新研究进展进行了综述,重点就AHAS的酶学特征、结构特征及结合方式,以AHAS为靶标的新颖除草活性化合物的设计开发以及AHAS抑制剂的抗菌生物活性研究进展等问题详细进行了总结,以期为设计开发靶向AHAS的新型除草剂或抗菌药物提供参考。 相似文献
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An attempt was made to account for quantitatively measured herbicidal performance of foliage-applied 5-hydroxy-3-methyl-2–oxo-imidazolidine-1-carboxamide derivatives by their photosynthesis-inhibiting activity and systemicity. Photosynthesis-inhibiting activity was estimated from the increase of chlorophyll fluorescence intensity in Chlorella vulgaris Beijer cells measured by a microplate scanner, and systemicity was also evaluated by computer-aided chlorophyll fluorescence imaging. The highest herbicidal performance was recorded for N-cyclohexyl-5-hydroxy-3-methyl-2-oxo-imidazo～idine-l-carboxamide, a compound with the second strongest photosynthesis-inhibiting activity and intermediate systemicity. Though neither photosynthesis-inhibiting activity nor systemicity showed significant correlation with the actual herbicidal performance in simple regression analyses, a high predictability was found for a multiple regression on both parameters as two independent variables, suggesting that these two factors work cooperatively in the field performance. 相似文献
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Andrea Occhipinti Łukasz Berlicki Samuele Giberti Gabriela Dziȩdzioła Paweł Kafarski Giuseppe Forlani 《Pest management science》2010,66(1):51-58
BACKGROUND: Aiming at the rational design of new herbicides, the availability of the three‐dimensional structure of the target enzyme greatly enhances the optimisation of lead compounds and the design of derivatives with increased activity. Among the most widely exploited herbicide targets is glutamine synthetase. Recently, the structure of a cytosolic form of the maize enzyme has been described, making it possible to verify whether steric, electronic and hydrophobic features of a compound are in agreement with inhibitor–protein interaction geometry. RESULTS: Three series of compounds (aminophosphonates, hydroxyphosphonates and aminomethylenebisphosphonates) were evaluated as possible inhibitors of maize glutamine synthetase. Aminomethylenebisphosphonate derivatives substituted in the phenyl ring retained the inhibitory potential, whereas variations in the scaffold, i.e. the replacement of the second phosphonate moiety with a hydroxyl or an amino residue, resulted in a significant loss of activity. A kinetic characterisation showed a non‐competitive mechanism against glutamate and an uncompetitive mechanism against ATP. A docking analysis suggested the mode of bisphosphonate binding to the active site. CONCLUSION: Results made it possible to define the features required to maintain or enhance the biological activity of these compounds, which represent lead structures to be further exploited for the design of new substances endowed with herbicidal activity. Copyright © 2009 Society of Chemical Industry 相似文献
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Ruling factors governing pre-emergence herbicidal activity were analysed for 16 photosynthesis-inhibiting 5-hydroxy-3-methyl-2–oxo-imidazolidine-1-carboxamide derivatives. Herbicidal performance was quantified by the reduction in area of experimental weed vegetation, measured by a computer-aided image analysis system. A system for fluorometric estimation of photosynthesis inhibitor concentration in aqueous solution greatly facilitated determination of the soil adsorption coefficients (Kd). Maximum herbicidal performance was found for N-sec-butyl-5-hydroxy-3-methyl-2-oxo-imidazolidine-1-carboxamide, a compound with the second lowest soil adsorptivity and average photosynthesis-inhibiting activity. A multiple regression analysis suggested that herbicidal performance of the soil-applied imidazolidine derivatives was determined by a balance between Kd and photosynthesis-inhibiting activity. In the present experimental system, however, the main influence was attributed to Kd. 相似文献
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Summary Populations of Setaria faberi and Digitaria sanguinalis cross-resistant to sethoxydim and fluazifop-P-butyl were identified in a vegetable cropping system in Wisconsin, USA, in 1991 and 1992 respectively. Experiments were conducted with partially purified acetyl-CoA carboxylase (ACCase) to determine whether resistance to sethoxydim and other ACCase inhibitors in S. faberi and D. sanguinalis resulted from altered enzyme activity. Based on I50 values (the herbicide dose that inhibited ACCase activity by 50% compared with untreated ACCase), ACCase of the resistant accession of S. faberi was 4.8-, 10.6- and 319-fold resistant to clethodim, fluazifop-P acid and sethoxydim, respectively, compared with that of the susceptible accession. Similarly, ACCase of the resistant accession of D. sanguinalis was 5.8-, 10.3- and 66-fold resistant to clethodim, fluazifop-P acid and sethoxydim respectively. These results indicated that resistance to ACCase inhibitors in these accessions of S. faberi and D. sanguinalis resulted from an altered ACCase enzyme that confers a very high level of resistance to sethoxydim. 相似文献
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The development of insects is under the control of a steroid hormone, ecdysone. This paper reviews suicide substrate type inactivators designed to inhibit the biosynthesis of ecdysone. Several series of acetylenic derivatives of cholesterol were synthesized and their biological effects on the prothoracic glands of the locust were investigated in vitro, enabling structure-activity relationships to be studied. Information on the ability of brassinosteroids, a series of plant growth regulators, to inhibit ecdysteroid activities of insects is discussed as a precursor to a study of brassinosteroid ecdysone mimics. 相似文献
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Mattia Liboni Łukasz Berlicki Paweł Kafarski Giuseppe Forlani 《Pest management science》2017,73(2):435-443
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Risk assessments for herbicides applied to roads are limited by the lack of knowledge on the fate and behaviour of the compounds in the urban environment. This study was designed to address this deficiency by quantifying the percentage loss of six herbicides following application to a roadside. Herbicides were applied on two occasions to a 16-m length of roadside and kerb edge. An automatic water sampler was used to collect run-off, draining to a single gulley pot, until 25 mm of rain had fallen. Samples were analysed for glyphosate, atrazine, diuron, oxadiazon and oryzalin, and peak concentrations were 650, 2210, 1810, 390 and 70 micrograms litre-1 respectively. Isoxaben was also applied, but concentrations in run-off were below the limit of detection (10 micrograms litre-1). Herbicide concentrations all followed a similar pattern of rapid decline throughout the first rain event following application, with the majority of loss occurring within the first 10 mm of accumulated rainfall, but compounds of high solubility and low Koc produced the highest peak concentrations. For those compounds of relatively low solubility and moderate Koc, application rate may be an influential factor in determining herbicide loss for these compounds. The percentage loss of the active substances applied differed between compounds, ranging from < 10% to 73%. The ecotoxicological significance of the results is discussed. 相似文献
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4种三唑类杀菌剂对黄瓜生长的影响 总被引：1，自引：0，他引：1
本文研究了在黄瓜幼苗期和三叶期施用4种三唑类杀菌剂对黄瓜生长的影响,幼苗期土壤浇灌结果表明:己唑醇和戊唑醇对黄瓜的影响作用相当且较明显,在12.5～200mg/L时,株高抑制率为25%～70%,己唑醇对根长的抑制率在20%～55%。丙环唑和腈菌唑对黄瓜的影响相对较弱,在50～200mg/L时,对株高的抑制率为10%～45%,在100～200mg/L时,对根长的抑制率仅为10%～15%。4种药剂对根鲜重均有明显的增加作用。三叶期茎叶喷雾处理结果显示,己唑醇和戊唑醇在25～100mg/L时,株高抑制率为15%～40%,丙环唑和腈菌唑50～100mg/L的株高抑制程度为5%～15%,4种药剂50～100mg/L对叶片叶绿素含量的增加在5%～30%。 相似文献