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1.
A newly synthesized experimental compound, EK-2612 is one of the class of cyclohexane-1,3-diones which are commonly known to be grasskillers. A greenhouse study was conducted to evaluate the herbicidal performances of EK-2612 on several grass species in comparison with tralkoxydim, a commercialized cyclohexanedione derivative. Like tralkoxydim, the compound EK-2612 showed excellent control efficacy on most grass weeds tested through foliar application rates between 250 and 63 g AI ha(-1). Unlike tralkoxydim, however, EK-2612 showed a good rice safety, and there was no rice damage observed at the level below 125 g AI ha(-1), while rice injury developed at the same application rates of tralkoxydim. With this rice safety, EK-2612 controlled barnyardgrass effectively up to the two-leaf stage under both submerged and dried paddy conditions. An in vitro ACCase assay indicated that EK-2612 is a strong ACCase inhibitor; however, the dose-response was not substantially different in rice and barnryardgrass, showing I50 values of 0.1 and 0.12 microM, respectively. These results suggest that the compound EK-2612 is targeting plant ACCase, but the whole-plant rice safety is not attributable to a different inhibition of the target site in rice from that in barnyardgrass.  相似文献   

2.
Fifteen 5-substituted 1-(6-chloro-3-pyridylmethyl)-2-nitromethylene-1,3- diazacyclohexanes and three other related compounds having a five- or seven-membered ring were synthesized and their biological activities were measured in vivo and in vitro. The insecticidal (in vivo) activity was evaluated against houseflies Musca domestica L under synergistic conditions with propargyl propyl phenyl phosphonate and piperonyl butoxide. The binding activity of each compound to nicotinic acetylcholine receptor in vitro was measured using [125I] alpha-bungarotoxin. The insecticidal activities of the unsubstituted diazacyclohexane analogues were slightly higher than those of the imidazolidine analogues, but the enlargement of ring size to diazacycloheptane lowered the activity. Substitution of 1,3-diazacyclohexane or imidazolidine rings was not generally favourable for the activity, but the unsubstituted 1,3-diazacyclohexane analogue showed the highest binding activity. Ring substitutions and ring enlargement decreased the activity 100-30,000-fold.  相似文献   

3.
BACKGROUND: 1,3‐Dichloropropene (1,3‐D, CAS No. 542‐75‐6) is a broad‐spectrum soil fumigant used to control numerous species of soilborne plant‐parasitic nematodes. 1,3‐D consists of two isomers, (Z)‐ and (E)‐1,3‐D. There are a number of low‐level chlorinated compounds that could potentially be produced as a part of the 1,3‐D manufacturing process. 1,3‐D and its metabolites, as well as potentially related chlorinated compounds, represent potential groundwater contaminants. RESULTS: This study has investigated the hydrolytic stability, under biotic and abiotic conditions in the laboratory, of an extensive representative list of 1,3‐D and potentially related chlorinated compounds in order to predict their environmental fate. All of these compounds showed intrinsic hydrolytic instability under both abiotic and biotic test conditions. Furthermore, a monitoring programme was carried out. Twenty‐five wells were monitored in five Italian regions characterised by historical and existing use of 1,3‐D. The parent compound, its two major metabolites and potentially related chlorinated compounds were not detected in the well water at > 0.1 µg L?1 at any sampling location. CONCLUSION: The soil fumigant (E,Z)‐1,3‐D, its metabolites and potentially related chlorinated compounds constitute a low risk to groundwater. Copyright © 2011 Society of Chemical Industry  相似文献   

4.
The extent of the risk of (Z)- and (E)-1,3-dichloropropene and their transformation products (Z)- and (E)-3-chloroallyl alcohol causing a hazard to the quality of groundwater pumped up for public water supply from below flower-bulb fields has been evaluated. The 1,3-dichloropropenes were incubated at 10°C in water-saturated subsoil material from three such fields. A first stage with gradual transformation was followed by a second stage with comparatively rapid transformation and after three months negligible amounts remained. The 3-chloroallyl alcohols were incubated at 15°C in soils from the root zone of the same fields. Complete transformation had occurred in about a week or even less. The 3-chloroallyl alcohols were also incubated in the water-saturated subsoil material at 10°C. Again, a first stage with gradual transformation was followed by a second stage with fast transformation. In most instances, the concentrations had fallen to a very low level within three months. It was concluded that it is unlikely that residues in the upper groundwater would permeate into the deeper groundwater pumped up for public water supply.  相似文献   

5.
Movement and biological activity of 1,3-dichloropropene (1,3-D) and chloropicrin applied through drip irrigation in raised beds was investigated at three locations in the southeastern USA. Tests were conducted in fields with dense populations of nutsedge (Cyperus spp), with one location also having a high level of soil nematodes, both of which served as biological indicators of the distribution of effective concentrations of 1,3-D and chloropicrin. Objectives were (1) to gain a better understanding of 1,3-D and chloropicrin movement and the extent of biological activity outside of the wetted bed area, and (2) to examine the effect of application rate, application concentration and subsequent irrigation events on movement and activity of 1,3-D and chloropicrin. InLine, an emulsifiable concentrate containing 60.8% w/w 1,3-D and 33.3% w/w chloropicrin, was injected into polyethylene mulched beds through the drip tubes and water movement in the beds was visualized by adding a blue dye to the injection system. Gas concentrations of 1,3-D and chloropicrin in soil were measured using Gastec detection tubes at different positions relative to the drip tube at 1-4 days after InLine application. After one week, mulch was removed and nutsedge survival evaluated at different positions in the bed. High concentrations of 1,3-D and chloropicrin were measured at the bed center and midway between the bed center and the shoulder, but concentrations were low at the bed shoulder. Width of nutsedge control was significantly greater than width of water movement. Plant-parasitic nematodes were controlled over the entire bed width, but nutsedge re-emerged at the bed shoulders regardless of treatment. Higher application rates and concentrations of 1,3-D + chloropicrin resulted in higher fumigant concentrations in soil air. Irrigations subsequent to application reduced soil air concentrations of 1,3-D and chloropicrin and increased water movement, as did the use of two drip tubes instead of one. The data show that the pesticidal activity of 1,3-D + chloropicrin extends beyond the waterfront and indicate a significant degree of fumigant activity of emulsifiable 1,3-D + chloropicrin. However, unlike plant-parasitic nematodes, nutsedge could not be controlled over the entire bed width, regardless of rate, concentration and volume of water applied.  相似文献   

6.
ABSTRACT The PaEXG2 gene, encoding an exo-beta-1,3-glucanase, was isolated from the biocontrol agent Pichia anomala strain K. PaEXG2 has the capacity for coding an acidic protein of 427 amino acids with a predicted molecular weight of 45.7 kDa, a calculated pI of 4.7, and one potential N-glycosylation site. PaEXG2 was disrupted by the insertion of the URA3 marker gene, encoding orotidine monophosphate decarboxylase in strain KU1, a uracil auxotroph derived from strain K. Strain KU1 showed inferior biocontrol activity and colonization of wounds on apples, compared to the prototrophic strain. Antagonism and colonization were recovered after the restoration of prototrophy by transformation with the URA3 gene. Integrative transformation was shown to be mostly ectopic in strain K descendants (only 4% of integration by homologous recombination). PaEXG2 disruption abolished all detectable extracellular exo-beta-1,3-glucanase activity in vitro and in situ but did not affect biocontrol of Botrytis cinerea on wounded apples.  相似文献   

7.
以亚甲二氧基苯为起始原料,经过溴化、硫化、环化等反应合成了19个未见文献报道的6,7-亚甲二氧基硫代苯并二氢吡喃-4-酮衍生物,其结构均经核磁共振氢谱和质谱确认。初步抑菌活性测试结果表明,在50 mg/L下,目标化合物对供试7种植物病原菌均有不同程度的抑制作用,其中化合物5b、5i、5k和5l对马铃薯干腐病菌 Fusarium solani的抑制率均达75%以上,5h和5i对番茄灰霉病菌Botrytis cinerea的抑制率分别是67.7%和70.4%。  相似文献   

8.
In addition to the molecular structure of a pesticide, environmental conditions may influence its persistence through their effect on the growth and activity of pesticide-degrading micro-organisms. As a result, transformation rates may decrease rapidly when a compound is leached into subsoil. Metamitron sorption isotherms were determined and incubation series were set up for a sandy loam soil, simulating single and combination effects that occur during transport of metamitron into subsoils. KOC values increased with increasing depth from 185 to 700 litre kg−1. A combination of conditions that are unfavourable for microbial activity, such as low temperature (5°C), low concentrations (0·5 mg kg−1) and a large sorbed fraction (KOC = 700) resulted in half-lives of over one year. Oxygen inhibition decreased the transformation rate of metamitron from 0·058 to 0·019 day−1. In order of significance, the transformation of metamitron appears to be a function of temperature, oxygen availability and sorption to organic carbon. Increasing doses did not change transformation rates significantly, although different transformation pathways were observed.  相似文献   

9.
10.
Benzpyrimoxan (5-(1,3-dioxan-2-yl)-4-{[4-(trifluoromethyl)phenyl]methoxy}pyrimidine, NNI-1501) was discovered as a novel insecticide structurally characterized by a pyrimidine derivative substituted with 1,3-dioxanyl and 4-trifluoromethylbenzyloxy groups. The compound showed remarkable activity against nymphs of rice planthoppers, including strains resistant to existing insecticides. Furthermore, benzpyrimoxan had low adverse effects on pollinators and beneficial arthropods. Because of these features, benzpyrimoxan is expected to be a suitable part of an integrated pest management strategy. In this report, the history of the discovery to reach benzpyrimoxan and details of the structure–activity relationships are described.  相似文献   

11.
为明确对羟苯基丙酮酸双氧化酶(HPPD)抑制剂类新化合物ZJ10361[1,3-二甲基-4-(2-甲基-4-甲砜基-3-(2-对甲苯氧基)乙氧基)苯甲酰基-1H-吡唑-5-基碳酸乙酯]在玉米田的开发应用潜力,对该化合物的除草活性、安全性、选择性、杀草谱和田间药效进行了研究。室内生物测定结果表明,ZJ10361在有效剂量150 g/hm2下对玉米安全性好,而对其他5种供试作物均有不同程度药害;对不同玉米品种之间的安全性有一定差异,其中对糯玉米科糯986安全性最好,其次为杂交玉米掖单13,甜玉米华珍最为敏感。该化合物在目标作物玉米Zea mays与反枝苋Amaranthus retroflexus、鳢肠Eclipta prostrata之间的选择性系数为4.0~4.5,具有较好的选择性;对阔叶杂草的除草活性较高,杀草谱较广,但对禾本科和莎草科杂草除草活性一般。田间试验结果显示,ZJ10361在有效剂量225 g/hm2下对供试玉米安全性好,对玉米田杂草总草防效为86.9%,与对照药剂硝磺草酮有效剂量150 g/hm2处理相比无显著性差异。该化合物用于玉米田防除阔叶杂草具有一定的开发潜力。  相似文献   

12.
The movement of 1,3-dichloropropene nematicides in 11 different field situations was monitored. The eventual dosages of 1,2-dichloropropane and 1,3-dichloropropene achieved at various positions in the soil profile are reported. Soil moisture, temperature, texture and profile differences are indicated for each experiment. The influence of soil profile modification, surface sealing techniques and various methods and rates of application are reported.  相似文献   

13.
为寻找新的环境友好型杀虫剂,用溴代呋喃甲醛和溴代噻吩甲醛分别与2-取代1,3-丙二硫醇缩合,合成了16个未见文献报道的2-溴代呋喃基或噻吩基-1,3-二噻烷衍生物。其化学结构均通过1H NMR和元素分析或质谱的确认。初步的生物活性测试结果表明,该类化合物对桃蚜Myzus persicae表现出一定的杀虫活性,其中化合物 M11 在600 μg/mL下对桃蚜的校正死亡率为90%。  相似文献   

14.
The rates of dissipation in soil and chloride-ion release, of the main components of dichloropropane-dichloropropene mixtures used as nematicides, were studied in sealed glass containers at different temperatures and moisture conditions. Half-lives of (Z)- and (E)-1,3-dichloropropenes at 20°C in soils were found to vary from 3 to 25 days; those of 1,2-dichloropropane and 2,3-dichloropropene were about four times and twice as long, respectively. The dissipation rates changed by a factor of about 2 per 10°C change in temperature. Judging from the release rates of waterextractable inorganic chloride in the soil (0-4% per week), the total degradation of all components applied at normal field rates was extremely slow. This indicated the formation of residues containing covalently bound chlorine. Only in ‘enrichment cultures’ was complete degradation indicated.  相似文献   

15.
为寻求具有较高生物活性的农药新品种,采用活性亚结构拼接法,以醛(1)为原料,经肟化、氯化反应,生成取代氯化肟类化合物(3),化合物3与炔螨特原药经1,3-偶极环加成反应,制得12个未见文献报道的目标化合物(ZJ1~ZJ12)。其结构均经过~1H NMR和MS确证。初步生物活性测定结果表明,在125 mg/L下,化合物ZJ12对朱砂叶螨Tetranychus cinnabarinus的致死率达75%,与炔螨特的杀螨活性相当;在200 mg/L下,化合物ZJ10对测试靶标的根、茎生长抑制率均为100%,优于对照药剂异丙酯草醚。  相似文献   

16.
The main objective of this study was to determine the influence of soil moisture, organic matter amendment and plastic cover (a virtually impermeable film, VIF) on diffusion and emissions of (Z)- and (E)-1,3-dichloropropene (1,3-D) in microplots of Florida sandy soil (Arredondo fine sand). Upward diffusion of the two isomers in the Arredondo soil without a plastic cover was greatly influenced by soil-water content and (Z)-1,3-D diffused faster than (E)-1,3-D. In less than 5 h after 1,3-D injection to 30 cm depth, (Z)- and (E)-1,3-D in air dry soil had diffused to a 10 cm depth, whereas diffusion for the two isomers was negligible in near-water-saturated soil, even 101 h after injection. The diffusion rate of (Z)- and (E)-1,3-D in near-field-capacity soil was between the rates in the two water regimes. Yard waste compost (YWC) amendment greatly reduced diffusion of (Z)- and (E)-1,3-D, even in air-dry soil. Although upward diffusion of (Z)- and (E)-1,3-D in soil with VIF cover was slightly less than in the corresponding bare soil; the cover promoted retention of vapors of the two isomers in soil pore air in the shallow subsurface. More (Z)-1,3-D vapor was found initially in soil pore air than (E)-1,3-D although the difference declined thereafter. As a result of rapid upward movement in air-dry bare soil, (Z)- and (E)-1,3-D were rapidly volatilized into the atmosphere, but emissions from the near-water-saturated soil were minimal. Virtually impermeable film and YWC amendment retarded emissions. This study indicated that adequate soil water in this sandy soil is needed to prevent rapid emissions, but excess soil water slows diffusion of (Z)- and (E)-1,3-D. Thus, management for optimum water in soil is critical for pesticidal efficacy and the environment.  相似文献   

17.
为了开发新的杀虫化合物,以氯虫苯甲酰胺为先导,2-甲基-3-氨基苯甲酸为起始原料,经过卤化生成5-氯-3-甲基-2-氨基苯甲酸;再与3-溴-1-(3-氯吡啶-2-吡啶基)-1H-吡唑-5-甲酸进行缩合反应,生成6-氯-2-(3-溴-1-(3-氯吡啶-2-吡啶基)-1H-吡唑-5-基)-8-甲基-4H-3,1-苯并噁嗪-4-酮;最后引入苯丙氨酸片段并经环化反应,分别合成了两个系列共计23 个新化合物( 4 和 5 ),其中化合物 4 为含苯丙氨酸的氯虫苯甲酰胺类似物,化合物 5 为由化合物4环化生成的含1H-茚-1-酮片段的氯虫苯甲酰胺类似物,所有化合物的结构均通过核磁共振氢谱(1H NMR)、碳谱(13C NMR)和高分辨质谱(HRMS)的表征及确证。初步室内杀虫活性测试结果表明,多数目标化合物对黏虫Mythinma separata具有较高的杀虫活性,其中14个化合物在100 mg/L下对黏虫Mythinma separata的致死率为100%,化合物 5k ( 1H-茚-1-酮片段中取代基为羟基 ) 在4和0.8 mg/L下的致死率分别为90%和70%,其LC50值为0.55 mg/L。分子对接结果表明,化合物 5k 与氯虫苯甲酰胺一样,也是作用于鱼尼汀受体(RyR),但与靶标结合的氨基酸残基不同,这种差异可能对黏虫的抗药性治理研究有益。  相似文献   

18.
Plastic films are used in soil fumigation to control fumigant emission into the atmosphere. In previous studies it was shown that the plastic films are permeable to fumigant vapors. Virtually impermeable films (VIF) have been developed to reduce such emission and to increase the efficacy of pest control. A rapid, accurate, sensitive and simple method to measure the permeability of plastic films to soil fumigants that was developed in the present study is described in this paper. The method uses a static, closed system in which the tested film is fixed between two cells. The fumigant is sampled by a solid-phase microextraction method and measured quantitatively by gas chromatography. The method was used to assess the permeability of two plastic films — a low-density polyethylene film (LDPE) and a VIF — to commercial soil fumigants formulated individually or in mixtures. All the tested fumigants permeated through the commonly used LDPE film, in the following descending order of permeability: methyl isothiocyanate (MITC), methyl bromide (MBr), 1,3-dichloropropene (1,3-D; Telone), chloropicrin (CP). The VIF was impermeable to all the tested fumigants except MITC, the permeation of which was reduced by 40%. The permeation of some fumigants through LDPE films was influenced by the formulation used. The permeation of CP was increased when it was combined with MBr in Bromopic. With Telopic, a mixture of 1,3-D and CP, the permeation of 1,3-D through LDPE film was 62% greater than that of Telone, whereas that of CP was not affected. The permeation rates of both MBr and CP were 25–30% greater when they were formulated as a mixture in Bromopic than when they were formulated individually. The formulation of fumigants as mixtures of two components did not affect their permeability through VIF. This study showed that differences in the suitability of plastic films for soil fumigation can be measured easily in a laboratory. It also showed that the VIP was more effective than LDPE in reducing losses of fumigant to the atmosphere, thus allowing more efficient use of fumigants to manage soilborne pests. The presented method helps us to choose the most adequate film for optimizing fumigation efficacy, and reducing costs and environmental risks. http://www.phytoparasitica.org posting Sept. 17, 2006.  相似文献   

19.
The performance of a newly developed column method for pesticide transformation rate measurements in the subsoil was tested using (Z)- and (E)-3-chloroallyl alcohol as model compounds. Sandy anaerobic water-saturated subsoil was collected at between 1·8 and 2·3 m below the surface of a flower-bulb field. Transformation rates were measured using subsoil columns that were filled in situ and were compared with the transformation rates in laboratory incubation systems. In the column experiment the half-life ranged from 0·5 to 5·2 days for (Z)-3-chloroallyl alcohol and from 1·0 to 5·5 days for (E)-3-chloroallyl alcohol. The capacity of the saturated subsoil for transformation of both isomers increased in the course of the column experiment. In the incubation experiment the 3-chloroallyl alcohols were transformed gradually in the first three days, with a half-life of 1·9 days for both isomers. Thereafter the transformation rate accelerated. The general conclusion is that the column method yields results similar to those of the incubation method for these rapidly transforming compounds.  相似文献   

20.
BACKGROUND: Preplant fumigation with methyl bromide (MeBr) has been used for control of soilborne pests in high‐value annual, perennial and nursery crops, but is being phased out. In 2007 and 2008, research trials were conducted to evaluate the effects of surface treatments and two application shanks on pest control with 1,3‐dicloropropene (1,3‐D) in perennial crop nurseries. RESULTS: All 1,3‐D treatments controlled nematodes similarly to MeBr. Application of 1,3‐D with virtually impermeable film (VIF) reduced Fusarium oxysporum compared with unfumigated plots, but was not as effective as MeBr. Applications of 1,3‐D with VIF or 1,3‐D followed by metam sodium reduced Pythium spp., but 1,3‐D followed by intermittent water seals was comparable with the untreated plots. When sealed with high‐density polyethylene (HDPE) film or VIF, 1,3‐D generally was as effective as MeBr for reducing weed density and total weed biomass, but weed control was reduced by intermittent water seals and in unsealed plots subsequently re‐treated with additional 1,3‐D or metam sodium. CONCLUSION: Applications of 1,3‐D sealed with HDPE or VIF film or with intermittent water seals can control nematodes similarly to MeBr. However, additional management practices may be needed for effective pathogen and weed control if plastic film is not used. Copyright © 2011 Society of Chemical Industry  相似文献   

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