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1.
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
2.
为了寻找结构新颖的琥珀酸脱氢酶 (SDH) 类衍生物,在前期发现吡唑联苯甲酰胺基础上,采用骨架跃迁的策略,设计并合成了18个N-取代苯基-4-(1-甲基-1H-吡唑-5-基) 噻吩-2-甲酰胺类衍生物 ( 3a~3n , 4a ~ 4d ),其中17个为新化合物。通过 1H NMR、13C NMR 和高分辨质谱 (HRMS) 确证了化合物的结构。离体杀菌活性测试结果表明:部分化合物对小麦赤霉病菌Fusarium graminearum、马铃薯早疫病菌Alternaria solani和草莓灰霉病菌 Botrytis cinerea 显示出较好的杀菌活性,其中化合物 3k 和 4d 对小麦赤霉病菌的EC50值分别为18.5和14.3 mg/L,化合物 4d 对马铃薯早疫病菌的EC50值为15.7 mg/L,活性略高于对照药剂噻呋酰胺 (EC50值27.8 mg/L),化合物 3k 和 3m 对草莓灰霉病菌的EC50值分别为15.3和 9.9 mg/L,与噻呋酰胺活性 (EC50值10.4 mg/L) 相当。分子对接研究结果显示:具有较高活性的化合物N-(4-氟苯基乙基)-4-(1-甲基-1H-吡唑-5-基) 噻吩-2-甲酰胺 ( 3m ) 与靶酶 (SDH) 的氨基酸残基之间存在较强的氢键作用。 相似文献
3.
The larvicidal and ovicidal effectiveness of twelve insecticides on Grapholita lobarzewskii Nowicki was tested by dipping apples in different concentrations of the insecticides. Emamectin was the most effective larvicidal product, with an LC(50) of 0.01 mg kg(-1), closely followed by spinosad, methoxyfenozide and chlorpyrifos-methyl, with LC(50) values between 0.2 and 0.7 mg kg(-1). Products like imidacloprid, indoxacarb, phosmet and thiacloprid gave LC(50) values between 1 and 2 mg kg(-1). Lastly, chlorpyrifos-ethyl and phosalone had LC(50) values of around 4 mg kg(-1), whereas tebufenozide and diflubenzuron had almost no larvicidal effect. Most of the products tested had low ovicidal effectiveness, and only fenoxycarb and emamectin gave LC(50) values worthy of note, close to 2 mg kg(-1). 相似文献
4.
A. Ian T. Walker Vernon K. H. Brown Jiro K. Kodama Ernest Thorpe Andrew B. Wilson 《Pest management science》1974,5(2):153-159
Acute and long-term mammalian toxicity studies were carried out with the 1,3,5-triazine herbicide cyanazine (I) and its two major plant and soil metabolites DW 43 85 (II) and DW 4394 (III). Depending upon the species used, the acute oral LD50 values for cyanazine ranged from 140-750 mg/kg, the values in any one species not being influenced by formulation. The acute, percutaneous LD50 values were greater than 1000 mg/kg, the maximum dose which could be administered. Cyanazine was non-irritant to eyes and skin and a non-sensitiser to skin. The acute oral LD50 in rats for (II) was 789 mg/kg and for (III) was >2000 mg/kg. In 13-week studies on cyanazine, reduced growth rates and organ weight changes were the most sensitive criteria of exposure, 25 parts/million in the diet of rats and 5 mg/kg orally dosed to dogs being considered to be without toxicological effect. In two year studies 12 parts/million in the diet of rats and 1.25 mg/kg, orally dosed to dogs produced no changes of toxicological significance. In 13-week studies with (II) and (III), intakes of up to 10 000 parts/million in the diet failed to produce any toxicologically significant changes. 相似文献
5.
Kan He Lu Zeng Qing Ye Guoen Shi Nicholas H. Oberlies Geng-Xian Zhao C. Jesse Njoku Jerry L. McLaughlin 《Pest management science》1997,49(4):372-378
The activities of 44 Annonaceous acetogenins, which were originally isolated by monitoring plant fractionations with the brine shrimp lethality test (BST), were evaluated in the yellow fever mosquito larvae microtiter plate (YFM) assay. The results clearly demonstrate that most acetogenins have pesticidal properties. The structure–activity relationships indicate that the compounds bearing adjacent bis-THF (tetrahydrofuran) rings with three hydroxyl groups are the most potent. Bullatacin ( 1 ) and trilobin ( 7 ) gave the best activities against YFM with LC50 values of 0·10 and 0·67 mg litre-1, respectively. Compounds showing LC50 values below 1·0 mg litre-1 in this assay are usually considered significant as new lead candidates for pesticidal development. In the BST, the corresponding LC50 values were 1·6×10-3 ( 1 ) and 9·7×10-3 ( 7 ) mg litre-1. This is the first report of pesticidal structure–activity relationships for a series of Annonaceous acetogenins which are known to act, at least in part, as potent inhibitors of mitochondrial NADH: ubiquinone oxidoreductase. © of SCI. 相似文献
6.
3种新型杀虫剂对苹果黄蚜的毒力效果评价 总被引：1，自引：0，他引：1
采用浸叶法在室内测定了3种药剂对苹果黄蚜的毒力,并在田间进行了防治试验。室内毒力测定结果表明:供试3种新型药剂中,双丙环虫酯和氟吡呋喃酮对苹果黄蚜的毒力较高,LC50分别为3.16 mg/L和23.58 mg/L,三氟苯嘧啶毒力较低,LC50为329.92 mg/L。田间试验结果表明:3种药剂对苹果黄蚜均有较好的速效性和持效性。17%氟吡呋喃酮可溶液剂和10%三氟苯嘧啶悬浮剂各处理3～7 d防效为82.19%～93.45%,药后30 d防效达到78.91%～87.92%;50 g/L双丙环虫酯可分散液剂2.5 mg/kg和4.2 mg/kg处理药后3～7 d防效为94.64%～97.04%,药后21 d防效仍可达88%以上。因此,3种新型药剂均可以用于防治苹果黄蚜,田间使用时推荐有效成分用量为双丙环虫酯2.5～4.2 mg/kg,氟吡呋喃酮113～170 mg/kg,三氟苯嘧啶28～80 mg/kg。 相似文献
7.
BACKGROUND: Because methyl bromide has been phased out as a soil sterilant, new nematicides are urgently needed. Four different chemical classes of organic acids acting as anion transport (AT) blockers were tested against a free-living nematode, Caenorhabditis elegans Maupas, a plant-parasitic nematode, Meloidogyne incognita (Kofoid and White) Chitwood, and an entomopathogenic nematode, Heterorhabditis bacteriophora Poinar, in toxicity bioassays. The materials tested were DIDS (4,4'-diisothiocyanatostilbene-2,2'-disulfonic acid), 9-AC (anthracene-9-carboxylic acid), NPPB [5-nitro-2-(3-phenylpropylamino)benzoic acid] and IAA-94 (indanyloxyacetic acid). RESULTS: All the compounds showed slowly developing nematicidal activity against second-stage juveniles of M. incognita and adults of C. elegans, but not against H. bacteriophora infective-stage juveniles. The LC(50) values of these compounds were < 50 mg L(-1) after 48 and 72 h incubation, while at 168 h incubation the LC(50) values were < 10 mg L(-1) for both sensitive species. Across both species and time, the LC(50) values generally differed no more than twofold among the four compounds tested in this study. In contrast, none of the compounds (200 mg L(-1)) caused more than control mortality to H. bacteriophora, even after 168 h of incubation. CONCLUSION: These compounds are potential leads for commercial nematicides. The insensitivity to H. bacteriophora is consistent with the natural exposure of this nematode to DST (3,5-dihydroxy-4-isopropylstilbene), a stilbene produced by its symbiotic bacterium. Based on the known activity of the compounds used in this study, it is suggested that anion transporters form the probable target sites for DIDS, 9-AC, NPPB and IAA-94 in nematodes. 相似文献
8.
Rabea EI Badawy ME Rogge TM Stevens CV Höfte M Steurbaut W Smagghe G 《Pest management science》2005,61(10):951-960
Chitosan, the N-deacetylated derivative of chitin, is a potential biopolysaccharide owing to its specific structure and properties. In this paper, we report on the synthesis of 24 new chitosan derivatives, N-alkyl chitosans (NAC) and N-benzyl chitosans (NBC), that are soluble in dilute aqueous acetic acid. The different derivatives were synthesized by reductive amination and analyzed by 1H NMR spectroscopy. A high degree of substitution (DS) was obtained with N-(butyl)chitosan (DS 0.36) at a 1:1 mole ratio for NAC derivatives and N-(2,4-dichlorobenzyl)chitosan (DS 0.52) for NBC derivatives. Their insecticidal and fungicidal activities were tested against larvae of the cotton leafworm Spodoptera littoralis (Boisduval) (Lepidoptera: Noctuidae), the grey mould Botrytis cinerea Pers (Leotiales: Sclerotiniaceae) and the rice leaf blast Pyricularia grisea Cavara (Teleomorph: Magnaporthe grisea (Hebert) Barr). The oral feeding bioassay indicated that all the derivatives had significant insecticidal activity at 5 g kg(-1) in artificial diet. The most active was N-(2-chloro-6-fluorobenzyl)chitosan, which caused 100% mortality at 0.625 g kg(-1), with an estimated LC50 of 0.32 g kg(-1). Treated larvae ceased feeding after 2-3 days; the mechanism of action remains unknown. In a radial hyphal growth bioassay with both plant pathogens, all derivatives showed a higher fungicidal action than chitosan. N-Dodecylchitosan, N-(p-isopropylbenzyl)chitosan and N-(2,6-dichlorobenzyl)chitosan were the most active against B cinerea, with EC50 values of 0.57, 0.57 and 0.52 g litre(-1), respectively. Against P grisea, N-(m-nitrobenzyl)chitosan was the most active, with 77% inhibition at 5 g litre(-1). The effect of different substitutions is discussed in relation to insecticidal and fungicidal activity. 相似文献
9.
为了发现具有生物活性的新化合物,以溴代吡咯腈为先导化合物,通过亲核取代等反应合成了一系列新型2-(溴代吡咯腈-1-基)乙酸衍生物(5a～5m, 6a～6o),其结构均经核磁共振氢谱(1H NMR)、碳谱(13C NMR)和高分辨质谱(HRMS)确证。杀菌活性测定结果显示：化合物2、3和5m对水稻稻瘟病菌Magnaporthe oryzae均表现出良好的杀菌活性,其EC50值分别为0.0532、0.0470和0.0174 mmol/L,优于对照药剂咯菌腈(0.0914 mmol/L),但不及对照药剂嘧菌酯(0.0001 mmol/L);化合物5m表现出一定的杀菌广谱性,其对水稻纹枯病菌Rhizoctonia solani和小麦根腐病菌Bipolaris sorokiniana的EC50值分别为0.0218和0.0420 mmol/L,但均不及对照药剂咯菌腈(EC50值分别为0.0002和0.0010 mmol/L)。杀虫、杀螨活性测定结果显示,在0.2 mmol/L浓度下,目标化... 相似文献
10.
白花丹根提取物的杀螨活性 总被引：18，自引：0，他引：18
研究了白花丹Plumbago zeylanica L. 根提取物对柑桔全爪螨的杀螨活性,发现其具有优良的杀螨、杀卵和产卵抑制活性.白花丹根先经甲醇冷浸提取,然后用石油醚萃取甲醇提取物,所得石油醚萃取物的12、24h杀螨致死中浓度(LC50)分别为2.52、2.12mg/ml, 产卵抑制中浓度(ODC50)分别为1.39、1.52mg/ml,杀卵LC50为1.04mg/ml.石油醚萃取物经硅胶柱层析后,以PE5-9馏份的活性最高,1mg/ml浓度下,杀螨率和杀卵率与白花丹素(plumbagin)标样在P=0.05水平均无显著差异.PE5-9馏份 12、24h的杀成螨LC50分别为0.71、0.67mg/ml,杀卵LC50为0.66mg/ml.不同溶剂展开系统薄层层析和GC-MS结果表明,该植物中的杀螨活性主要成分为白花丹素. 相似文献
11.
采用超高效液相色谱-串联质谱法(UPLC-MS/MS),优选最佳QuEChERS样品前处理方法,建立了紫花地丁Viola yedoensis中82种农药残留的快速筛查和定量检测方法。通过正交试验设计9种组合,研究4种不同吸附剂(PSA、C18、GCB和SiO2)对紫花地丁净化效果的影响。紫花地丁样品分别经800 mg PSA、3 200 mg C18、1 600 mg GCB和1 600 mg SiO2提取与净化,采用phenomenex DOD-4475-AN C18色谱柱分离,0.1%甲酸(含10 mmol/L甲酸铵)-乙腈混合溶液进行梯度洗脱,标准曲线法定量。结果表明:82种农药在相应的线性范围内,色谱响应值与对应的质量浓度间均呈良好的线性关系(r ≥ 0.99),检出限(LOD)均在0.3~5 μg/kg之间,定量限(LOQ)均在1~20 μg/kg之间。在0.02、0.05和0.1 mg/kg 3个添加水平下,大多数农药的平均回收率介于70%~111%之间,相对标准偏差(RSD,n = 6)小于19%。该方法操作简单、准确、高效,可满足紫花地丁中82种农药残留同时检测的要求。 相似文献
12.
The activity of rhodojaponin-III (R-III), a grayanoid diterpene compound isolated from Rhododendron molle G. Don flowers, was determined under laboratory and field conditions as an antifeedant, stomach poison, contact toxicant and insect growth inhibitor against Pieris rapae (L.) larvae. The median antifeedant concentration (AFC(50)) values in no-choice leaf disc tests were 1.16 and 15.85 mg L(-1) at 24 h after treatment when tested against third and fifth instars respectively. The median lethal concentration (LC(50)) values in leaf disc tests were 2.84 and 9.53 mg L(-1) at 96 h after treatment against third and fifth instars respectively. R-III showed an almost 30 times higher contact toxicity against third instars than for fifth instars, and the median lethal dose (LD(50)) values for topical application were 1.18 and 34.09 mg kg(-1) at 72 h after treatment respectively. R-III disrupted the development of larvae to pupae or adults with median concentration for inhibiting growth (IC(50)) values of only 1.36 mg L(-1) for third instars and 11.28 mg L(-1) for fifth instars. In field trials, a greater than 80% reduction in the adjusted larval numbers was obtained against P. rapae 14 days after treatment when Rhodo 0.1% EC, a commercial botanical insecticide based on R-III, was applied at both 937.5 and 625 mL ha(-1). These results suggest that further research to develop R-III, and extracts from R. molle, as biorational pesticides or as lead compounds for integrated pest management deserve consideration. 相似文献
13.
9种杀菌剂对西瓜炭疽病菌的室内毒力测定及配比试验 总被引：3，自引：0，他引：3
为筛选防治西瓜炭疽病的高效低毒杀菌剂, 缓解和治理生产中病菌对药剂的抗性, 在室内离体条件下采用生长速率抑制法及孢子萌发抑制法测定了9种杀菌剂对西瓜炭疽病菌( Colletotrichum orbiculare )的毒力。结果表明, 嘧菌酯、咪鲜胺和甲基硫菌灵对病原菌菌丝生长的EC50在0.093 3~0.118 2 mg/L之间, 均小于1 mg/L, 表明西瓜炭疽病菌对上述杀菌剂比较敏感; 百菌清、烯肟菌酯和戊菌唑的EC50在2.310 1~5.925 9 mg/L, 病菌对药剂的敏感程度相对较低; 代森锰锌、恶霉灵和多菌灵的EC50分别为36.876 3、74.466 6和99.898 5 mg/L, 抑菌活性较差。孢子萌发试验中, 嘧菌酯、咪鲜胺和甲基硫菌灵对病菌孢子萌发的抑制活性最高, EC50在0.069 4~0.167 2 mg/L之间; 百菌清、烯肟菌酯、代森锰锌的抑制活性次之, EC50在1.853 0~9.503 9 mg/L之间; 多菌灵的抑制活性相对最低, EC50为99.335 3 mg/L。将两种不同作用机理的杀菌剂嘧菌酯与咪鲜胺按照2∶1的比例混配, 联合毒力测定和评价结果表明两者混配对抑制西瓜炭疽病菌具有增效作用。 相似文献
14.
Benzhydrolpiperidine (BZP) insecticides represent a novel class of chemistry. Their specificity and efficacy as well as their low mammalian toxicity give them excellent potential for commercialization. Several N-arylalkylbenzhydrolpiperidines were tested for activity against a variety of insects in the laboratory and greenhouse. These tests were used to select compounds for field trials and determine rates of application for field tests. The BZP compounds have good activity against Lepidoptera, with modest Coleoptera activity. They are toxic by oral administration and have about 100-fold lower activity by topical exposure. A methyl carbamate BZP, F4265, was the most active compound, with LC50 values of 6 mg litre(-1) or less for most Lepidopteran species tested. F4265 was active in a variety of field trials at 112-224gAI ha(-1). Whole-plant testing methods conducted in the greenhouse were effective in determining field test rates. 相似文献
15.
Kreutzweiser DP Good KP Chartrand DT Scarr TA Holmes SB Thompson DG 《Pest management science》2008,64(2):112-118
BACKGROUND: Imidacloprid is an effective, systemic insecticide for the control of wood-boring insect pests in trees. Systemic applications to trees are often made by soil injections or drenches, and the resulting imidacloprid concentrations in soil or litter may pose a risk of harm to natural decomposer organisms. The authors tested effects of imidacloprid on survival and weight gain or loss of the earthworms Eisenia fetida (Savigny) and Dendrobaena octaedra (Savigny), on leaf consumption rates and cocoon production by D. octaedra and on microbial decomposition activity in laboratory microcosms containing natural forest litter. RESULTS: Dendrobaena octaedra was the most sensitive of the two earthworm species, with an LC(50) of 5.7 mg kg(-1), an LC(10) of about 2 mg kg(-1) and significant weight losses among survivors at 3 mg kg(-1). Weight losses resulted from a physiological effect rather than from feeding inhibition. There were no effects on cocoon production among survivors at 3 mg kg(-1). The LC(50) for E. fetida was 25 mg kg(-1), with significant weight losses at 14 mg kg(-1). There were no significant effects on microbial decomposition of leaf material at the maximum test concentration of 1400 mg kg(-1).CONCLUSION: The results indicate that, when imidacloprid is applied as a systemic insecticide to the soil around trees, it is likely to cause adverse effects on litter-dwelling earthworms if concentrations in the litter reach or exceed about 3 mg kg(-1). 相似文献
16.
The toxic effects of permethrin and ten of its degradation products on the growth of ten fungi were determined. Permethrin was relativelynon-toxic, with an EC50 of > 100 mg litre?1 but six of the degradation products were significantly (P= 0.05) more inhibitory. The ester hydrolysis products, 3-phenoxybenzyl alcohol and 3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropanecarboxylic acid, had EC50 values ranging from 8 to > 100 and 20 to > 50 mg litre?1, respectively. Other degradation products that were more toxic than permethrin included 3-phenoxybenzaldehyde and 3-phenoxybenzoic acid, with EC50 values as low as < 1 mg lite?1. Hydroxylated and substituted-benzene metabolites were non-toxic. Combinations of selected test compounds yielded both synergistic, antagonistic and additive interaction responses, depending upon the test system employed. 相似文献
17.
Three rearranged phragmalin-type limonoids, khayanolide A, khayanolide B and 1-O-acetylkhayanolide B, and a mexicanolide-type limonoid, khayalactol, have been isolated from the stem bark of Khaya senegalensis (Desr) A Juss (Meliaceae). The antifeedant and growth-inhibitory activities of the isolated compounds were evaluated on Spodoptera littoralis (Boisduval). When added to an artificial diet, khayanolide A, khayanolide B and 1-O-acetylkhayanolide B showed antifeedant activity in a concentration-dependent manner. Khayalactol exhibited strong antifeedant activity without significant differences at all of the tested concentrations (7.5-100 mg kg(-1)). Khayanolide B was the most potent antifeedant with an ECso of 2.19 mg kg(-1). The results also revealed that the isolated compounds caused marked larval growth inhibition on S littoralis after 7 days of feeding on treated diet; this effect was concentration-dependent. Khayanolide B was the most active growth inhibitor among the isolated compounds, with an EC50 of 6.96 mg kg(-1). 相似文献
18.
Donald E. Clegg 《Pest management science》1974,5(6):769-779
A series of trials in which cattle were either treated dermally or dosed orally with clenpirin [2-(3,4-dichlorophenylimino)-l-n-butyl pyrrolidine] was undertaken. Tissue fat from steers and butter fat from milking cattle were sampled and residue levels determined colorimetricaliy. Residues following a single application of clenpirin (9 litres/beast at 0.25% w/v) reached an average maximum of 2.0 mg/kg in body fat and then declined to 0.2 mg/kg after 14 days. Multiple applications (9 litres/beast at 0.25% w/v) resulted in a progressive buildup of residues in body fat to about 30 mg/kg after 4 treatments. When steers were dosed orally with technical clenpirin at 700 mg/beast/day for 15 days the average fat level reached 0.7 mg/kg. In a series of trials with milking cattle a single dermal exposure (0.23-0.3% w/v aqueous emulsion) yielded residues in butter fat ranging from 1 5.5-51 1 mg/kg at the first sampling 5 h after treatment. Six days later these had declined to about 0.8 mg/kg. 相似文献
19.
Field dissipation, soil movement and laboratory leaching studies were performed to elucidate the effect of two rainfall amounts in the behaviour and environmental fate of simazine under climatic conditions at Casablanca Valley, Chile. Dissipation and soil movement were studied in a field vineyard with a sandy loam soil (Inceptisol; 74.08% sand; 14.87% silt and 11.04% clay). Simazine was applied to bare soil at 2.0 kg AI ha(-1), and its concentration was measured using immunoassay (ELISA) at 0, 10, 20, 40 and 90 days after application under two rainfall amounts, natural field conditions (39 mm) and modified conditions (39 + 180 mm). Simazine leaching was studied using soil core PVC lysimeters (0.9 m height; 0.22 m diameter). Field dissipation data were adjusted with a bi-exponential model. Half-life (DT(50)) values varied between 31.3 (+/-2.5) and 19.0 (+/-4.2) days under natural and modified conditions, respectively. Simazine K(d) varied from 0.42 to 2.15 (K(oc) 32.6-216.2) in the soil profile. Simazine was detected at a 90-cm soil depth in concentrations of 0.0085 (+/-0.0043) mg kg(-1) and 0.0321 (+/-0.001) mg kg(-1) under field and modified conditions, respectively. The maximum simazine leachate concentrations were 0.013 (+/-0.00084) mg litre(-1) (0.012% of total applied simazine) and 0.0084 (+/-0.00082) mg litre(-1) (0.11% of total applied simazine) for field and modified conditions respectively. These data indicate that water quantity has a significant effect on the DT(50) and the amount of simazine that moved through the soil profile, but not on the soil depth reached by this herbicide. 相似文献
20.
An artificial soil test was used to determine the LC50 values of carbaryl, chlorpyrifos, imidacloprid, cyfluthrin and fipronil against earthworms of the Pheretima group. For a 24-h interval, carbaryl was the most toxic to earthworms (LC50 = 77 mg kg-1), followed by imidacloprid (155 mg kg-1), cyfluthrin (351 mg kg-1), chlorpyrifos (390 mg kg-1) and fipronil (> 8550 mg kg-1) as the least toxic. For the 48-h and 7-day intervals, imidacloprid was the most toxic to earthworms (LC50 = 5 mg kg-1 and 3 mg kg-1 respectively), followed by carbaryl (16 mg kg-1; 9 mg kg-1), cyfluthrin (128 mg kg-1; 110 mg kg-1), chlorpyrifos (330 mg kg-1; 180 mg kg-1) and the least toxic was fipronil (> 8550 mg kg-1 both intervals). The surface application rates required to achieve these values are compared with the rates recommended for the control of turfgrass pests. 相似文献