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1.
A new compound 3-(3-bromothiophen-2-yl)-5-(2,6-difluorobenzyl)oxymethyl-5-methyl-4,5-dihydroisoxazole was synthesized and the herbicidal activity was assessed under glasshouse and flooded paddy field conditions. This compound demonstrated good rice selectivity and potent herbicidal activity against annual weeds at 125 g ai ha−1 under greenhouse conditions. Soil application of this compound showed the complete control of barnyardgrass to the 4th leaf stage at 250 g ai ha−1. Field trials indicated that this compound, combined with pyrazosulfuron-ethyl, controlled annual and perennial weeds rapidly with good tolerance by transplanted rice seedlings from postemergence and soil application. This compound showed a low mammalian and environmental toxicity in various toxicological tests.  相似文献   

2.
Novel tricyclic 3,3a,5,9b-tetrahydro-2H-furo[3,2-c][2]benzopyran (TFB) derivatives were synthesized, and their herbicidal activities were elucidated. They were synthesized from D-glucose as a natural chiral source. The formation of the TFB skeleton was achieved by a Friedel-Crafts type intramolecular cyclization of methyl 5-deoxy-2,3-O-dibenzyl-5-C-methyl-D-xylofranosides. The intramolecular cyclization was dependent upon the electronic effects of the substituents at the C-2 benzyloxy group of methyl xylofranosides. Some TFBs exhibited a remarkable herbicidal activity to annual paddy weeds, such as Echinochloa sp, without injury to the rice.  相似文献   

3.
A number of 6-(4-phenoxyphenoxy)pyrimidines and triazines were synthesized and their herbicidal activity was measured. Compounds with the methoxy groups at the 2- and 4-positions on the pyrimidine and triazine rings exhibited high herbicidal activity. Introduction of a substituent into the 5-position of the pyrimidine ring diminished the activity. In the phenoxyphenoxy substructure at the 6-position, the central ether bond can be replaced by a methylene group without loss of activity. The optimum substituent on the terminal phenyl ring was 3-trifluoromethyl. The compounds showed a strong Hill reaction inhibition, but unfortunately showed poor selectivity between weeds and crops.  相似文献   

4.
Alkyl 3-benzoyl-3-(3-chloro-4-substituted-phenyl)-2-methylcarbazates (isoelectronic analogues of wild oat herbicides) have plant growth regulating properties for various weeds and crops. Some derivatives of carbazates, bearing halogen in the 4-position of the phenyl group, have been shown to have the highest activity of the prepared compounds.  相似文献   

5.
双环磺草酮除草活性及对水稻的安全性研究   总被引:1,自引:1,他引:0  
双环磺草酮是一种以对-羟苯基丙酮酸双氧化酶 (HPPD) 为作用靶标的双环辛烷类化学除草剂。为明确其在水稻田的应用技术,采用温室盆栽法测定了双环磺草酮的杀草谱、除草活性及对8个水稻品种的安全性。结果表明:在有效成分360 g/hm2剂量处理下,双环磺草酮对水稻田常见杂草稗草Echinochloa crusgalli、雨久花Monochoria korsakowii、异型莎草Cyperus difformis的地上部分鲜重抑制率均高于90%,对主要秋熟杂草稗草E. crusgalli、牛筋草Eleusine indica、雨久花M. korsakowii、千金子Euphorbia lathyris、田皂角Aeschynomene indica和异型莎草C. difformis的GR50值为有效成分48~196 g/hm2,除田皂角外,除草活性均高于对照药剂硝磺草酮。双环磺草酮对8个水稻品种的安全性研究结果表明:在有效成分720 g/hm2剂量处理下,隆两优华占、皖垦糯1号、皖稻68和绿旱粳1号4个水稻品种对双环磺草酮耐药性较高,徽两优882、C两优608、皖稻119和Y两优1号4个水稻品种的株高和鲜重受到不同程度的抑制。双环磺草酮在隆两优华占、皖垦糯1号、皖稻68和绿旱粳1号4种水稻与异型莎草、稗草和雨久花3种杂草之间的选择性指数分别为3.66~4.37、4.50~5.37、3.36~4.01和3.29~3.93,明显高于对照药剂硝磺草酮。研究表明,双环磺草酮对多种秋熟杂草防效较好,且对供试的3个粳稻品种及5个籼稻品种中的隆两优华占安全。  相似文献   

6.
A new series of the O-pyrimidinylsalicylates was synthesized and their herbicidal activity was examined. Some of these compounds showed very strong herbicidal activity under pre- and post-emergent treatment conditions against various kinds of grass and broadleaf weeds. Among these compounds, O-(4, 6-dimethoxypyrimidin-2-yl) salicylic acid and its methyl ester were found to exhibit the highest activity. The herbicidal symptoms observed after the treatments included early cessation of plant growth followed by chlorosis, necrosis and plant death. The symptoms were similar to those caused by sulfonylureas and imidazolinones, which inhibit branched-chain amino acid biosynthesis.  相似文献   

7.
以2,5-二羟基苯甲酸甲酯和三氟羧草醚为起始原料,设计合成了3个系列20个新的三氟羧草醚类似物,通过核磁共振氢谱、碳谱对其结构进行了表征。分别采用小杯法和室内盆栽法测定了目标化合物的除草活性。结果表明,化合物 III-02 [5-(2-氯-4-三氟甲基苯氧基)-2-硝基苯甲酸-(6-甲基苯并噻唑-2-基)酯]对单子叶杂草的除草活性明显高于对照药剂三氟羧草醚,其对稗草Echinochloa crusgalli和马唐Digitaria sanguinalis根茎生长的EC50值分别为2.03、0.93 μg/mL和1.49、0.52 μg/mL;在有效成分100 g/hm2的施药剂量下,化合物 III-02 对单子叶杂草稗草、马唐及狗尾草Setaria viridis的防治效果均在85%以上,明显高于三氟羧草醚,对阔叶杂草马齿苋Portulaca oleracea、反枝苋Amaranthus retroflexus及苘麻Abutilon theophrasti的防治效果可达100%。初步构效关系表明,2-硝基苯甲酰衍生物的除草活性明显优于其2-甲氧基衍生物,三氟羧草醚苯甲酸酯衍生物对单子叶杂草的除草活性明显高于其苯甲酰胺衍生物。  相似文献   

8.
A series of novel alpha,alpha,alpha-trifluoro-m-tolyl pyridazinone derivatives was synthesised. Herbicidal activities of the two intermediate compounds and 15 pyridazinone derivatives were evaluated through barnyardgrass and rape cup tests and Spirodela polyrrhiza (L.) Schleiden tests. Selected compounds were also evaluated under greenhouse conditions. Bleaching activities were observed at 10 microg ml(-1) and some compounds exhibited herbicidal activities at a rate of 300 g ha(-1). The relationship between crystal structures and herbicidal activities is discussed through a comparison of two compounds (5a and 5f).  相似文献   

9.
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   

10.
1-Phenyl-5(4 H )-4-dialkylcarbamoyltetrazolinones represent a new class of herbicides that are active against barnyardgrass ( Echinochloa spp.) in paddy fields. To select the most favorable compound as a paddy herbicide, herbicidal activity and selectivity of the carbamoyltetrazolinone compounds to transplanted rice were determined in greenhouse tests. Higher herbicidal activities were associated with the compounds having a 2-Cl- or 2-Cl-6-Me-substituted or an unsubstituted phenyl ring, and a combination of C2–3 linear alkyl group and a C4 branched-chain alkyl or a C5–6 cycloalkyl group on the nitrogen atom in the carbamoyl structure. In addition, the compounds carrying a total of seven to nine carbon atoms in the substituents on the carbamoyl nitrogen exhibited a good selectivity between barnyardgrass and transplanted rice plants. From the results of soil thick-layer chromatography, the good crop compatibility of carbamoyltetrazolinones was correlated to the mobility of the compounds in paddy soil. The investigation resulted in the selection of an excellent compound, 4-(2-chlorophenyl)- N -cyclohexyl- N -ethyl-4,5-dihydro-5-oxo-1 H -tetrazole-1-carboxamide (common name: fentrazamide), as a rice paddy herbicide for controlling barnyardgrass.  相似文献   

11.
双环磺草酮是一种新型的对羟基苯丙酮酸双加氧酶抑制剂类除草剂,为明确其除草活性以及其与合成激素类除草剂氯氟吡啶酯复配后的除草效果,采用温室盆栽法研究了二者复配的联合作用类型,以及复配药剂在水稻与杂草之间的选择性,并进行了田间药效评价。温室盆栽试验结果表明:双环磺草酮与氯氟吡啶酯复配后使用,对供试杂草稗草、千金子、异型莎草及鸭舌草均呈现加成或增效作用;其中二者按照质量比5:1复配后的除草活性高于双环磺草酮单剂;复配药剂在供试水稻品种与杂草之间的选择性指数在28.72~54.81之间,与两种单剂相比,复配药剂对水稻的安全性均有提高。田间药效试验结果表明:双环磺草酮与氯氟吡啶酯复配扩大了杀草谱,对稗草、千金子、异型莎草及雨久花的株防效和鲜重防效在93.4%~100%之间,且对水稻安全;其中,田间复配用量为双环磺草酮有效成分120 g/hm^2、氯氟吡啶酯有效成分18 g/hm^2时效果最佳,对4种供试杂草的防效为97.1%~100%。  相似文献   

12.
为了明确新型除草剂NC1的杀草谱、施药时期、使用剂量及对水稻的安全性,采用种子生物测定法测定34.5% NCI悬浮剂对稗草的生物活性,并与30乡丙草胺乳油进行比较;采用室内整株生物测定法测定34.5%NC1 SC不同时期处理对禾本科杂草的控制作用和对水稻的安全性,并进行田间验证.结果 表明:NC1对稗草种子的生物活性优...  相似文献   

13.
为了研究2-仲丁氨基-5-(2-氯吡啶-4-基)-1,3,4-噻二唑(BCPT)的结构-活性关系和开发活性更高的新型除草剂,以BCPT为先导化合物,依据活性亚结构连接法,在吡啶环2-位上引入二芳醚类除草剂的典型结构单元——芳醚,设计并合成了一系列新的芳氧吡啶噻二唑类化合物,其结构经元素分析和1H NMR确证。初步除草活性测定结果表明,在500 mg/L剂量下,所有化合物的除草活性(抑制率0~45%)远低于先导化合物(抑制率72%~87%),说明吡啶环2-位上的氯原子可能对维持该类化合物的除草活性是必需的。  相似文献   

14.
新型除草剂ZJ0862的研究与开发   总被引:2,自引:0,他引:2  
以水杨醛、3,4-二氯苯胺和4,6-二甲氧基-2-甲砜基嘧啶为原料合成了新型除草剂ZJ0862 ,其结构经1H NMR、MS、IR和元素分析确证。室内生物测定试验表明,ZJ0862在有效成分60 g/hm2剂量下,对水田重要杂草稗草和异型莎草的抑制率达90%以上;在45 g/hm2剂量下,对看麦娘、野燕麦、狗尾草等15种田间常规杂草的抑制率达85%~100%,杀草谱较广;田间试验结果显示,ZJ0862在150 g/hm2剂量下对移栽水稻安全,且在 60~90 g/hm2剂量下对水田主要杂草水苋菜、陌上菜、异型莎草等的防效达81.3%~98.4%。毒理学评价结果显示,该药剂为低毒、无刺激、弱致敏和致突变阴性。ZJ0862具有高效、低毒、安全的特点,在移栽水田将具有较好的开发前景。  相似文献   

15.
The new benzenesulfonylurea K-11451, an α-hydroxy-β-fluoropropyl- compound, applied at 3–9 g ha −1, controlled annual and perennial weeds grown in submerged paddy soil under greenhouse conditions. It effectively controlled barnyardgrass at growth stages varying from pre-emergence to the five-leaf stage. The compound inhibited acetolactate synthase, I50 values for the enzyme isolated from barnyardgrass and rice being 56 and 67 nM , respectively. K-11451 inhibited the growth of rice when it was transplanted at a shallow depth (0–1 cm) and water leaching from the paddy soil was high (3–5 cm per day). With a water depth of 3 cm, the compound appeared to move readily down into the paddy soil and had the relatively short half-life of 15.2 days under submerged paddy conditions. A mixture of K-11451 + mefenecet + daimuron (9 + 250 + 250 g ha−1) controlled almost all weeds in the paddy field without injury to rice, so that the combination could be used as a ‘one-shot’ herbicide in rice culture.  相似文献   

16.
Summary. Several new herbicides were tested for control of weeds in broadcast-seeded flooded tropical rice. Among the new herbicides, S-(2-methyl-l-piperidylcarbonyl-methyl)- O,O -di- n -propyl dithiophosphate (C-19490), S-(2-methyl-l-piperidylcarbonyl-methyl)- O,O -di- n -propyl dithiophosphate combined with 2-(1',2'-dimethylpropylamino)-4-ethylamino-6-methylmercapto- s -triazine [C-19490/C-18898 (C-288)], and N -secondary-butyl-4-tertiary-butyl-2,6-dinitroaniline (A-820) were highly selective in controlling Echinochloa crus-galli (barnyard grass) and other annual weeds under tropical conditions. S-(4-chlorobenzyl)- N,N -diethylthiol carbamate (benthiocarb) and N -(butoxymethyl)-2-chloro-2',6'-diethylacetanilide (butachlor) continued to look promising in our experiments. Only butachlor is widely used in Asia.
Désherbage chimique des cultures tropicales de riz inorndé, seméà la volée  相似文献   

17.
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   

18.
Bentazon, 3-isopropyl-2,1,3-benzothiadiazin-4-one-2,2-dioxide is effective for weed control in flooded rice fields not only as a foliar treatment but also as a flooded-water or paddy soil treatment. Generally the herbicidal effect develops slowly only after translocation of the herbicide has occurred, but when the weeds contacted directly with relatively high concentrations of the herbicide, the effects appear rather rapid.The slow herbicidal effect appears to be an important mode of action of bentazon applied practically on weeds under flooded rice field conditions. The slow effect may be caused by inhibition of photosynthesis as supported by the following experimental results: a) Bentazon inhibited the Hill reaction in isolated chloroplasts; b) bentazon rapidly inhibited photosynthetic CO2 fixation in susceptible Cyperus serotinus and other plants; c) the herbicidal effects appeared much slower when bentazon was applied as a flooded-water treatment; d) bentazon injury was prevented by endogenous or exogenously supplied carbohydrates.  相似文献   

19.
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.  相似文献   

20.
Three field trials were conducted from 2003–2004 at Utsunomiya University, Japan, to evaluate the safety and herbicidal activity of pyribenzoxim (benzophenone O -[2,6-bis[(4,6-dimethoxy-2-pyrimidinyl)oxybenzoyl]oxime) in turfgrass. Pyribenzoxim showed a high level of safety in bentgrass ( Agrostis palustris Huds.) and zoysiagrass ( Zoysia matrella ) ≤ 300 g ai ha−1 and it controlled various major grass weeds, including annual bluegrass ( Poa annua L.), large crabgrass ( Digitaria sanguinalis L.), and green foxtail ( Setaria viridis L.), and broadleaf weeds, including common dandelion ( Taraxacum officinale Weber), horseweed ( Erigeron canadensis L.), shepherd's-purse ( Capsella bursa-pastoris (L.) Medic.), common chickweed ( Stellaria media L.), common lambsquarters ( Chenopodium album L.), creeping woodsorrel ( Oxalis corniculata L.), and common dayflower ( Commelina communis L.) by fall or spring application. In comparison with bispyribac-sodium (sodium 2,6-[bis(4,6-dimethoxy-2-pyrimidin-2-yl)oxy]benzoate), pyribenzoxim showed a higher safety level in bentgrass and a stronger herbicidal activity on grass weeds; in particular, annual bluegrass and large crabgrass.  相似文献   

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