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1.
Chemical modification of the herbicide 1-[2-(benzothiazol-2-yl)isopropyl]-4-methyl-3-phenyl-5H-pyrrolin-2-one (MI-2826) has revealed a new oxazinone herbicide, 3-[2-(7-chlorobenzothiazol-2-yl)isopropyl]-2,3-dihydro-6-methyl-5-phenyl-4H-1,3-oxazin-4-one (MI-3069), for use in paddy fields. In comparing the phyototoxicity of the two herbicides to transplanted rice, the latter was superior to the former and kept the same predominant characteristic to control Echinochloa oryzicola Vasin for a long period of time owing to its long-lasting residual effect. 相似文献
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Piperonyl butoxide (PB) is a known Synergist which enhances the activity of insecticides by inhibiting their biotransformation
to less active products. We have evaluated the possible use of PB as a herbicide synergist using triazine herbicides in sensitive,
tolerant, and resistant plants. The effects of PB, triazine herbicides, and their combinations were examined in whole plants
as well as in chloroplasts isolated from triazine-sensitive (S) and -resistant (R) weed biotypes. PB itself, applied postemergence
(0.1–0.5%, v/v), was slightly toxic to the plants tested. However, foliar application of PB combined with atrazine, terbutryn
or prometryn to maize seedlings significantly increased the phytotoxicity of the herbicides. Low rates of atrazine, prometryn,
and terbutryn in a tank-mixture with PB, effectively controlled Solatium nigrum L. and Abutilon theophrasli Medik. PB enhanced
atrazine efficacy in both S and R biotypes of Lolium rigidum Gaud. The synergistic effect of PB was evident also in vitro
when atrazine and methabenzthiazuron were used to inhibit photosystem II electron transport in chloroplasts isolated from
resistant weeds. These data demonstrate the potential of PB as a herbicide synergist and its possible utilization as an aid
for improving the activity of triazine herbicides in sensitive, tolerant and resistant plants. 相似文献
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Young Kwan Ko Dong Wan Koo Hae Sung Chang Jae Wook Ryu Jae Choon Woo In Taek Hwang Kyung Sik Hong Jin-Seog Kim Kwang Yun Cho Dae-Whang Kim 《Pest management science》1999,55(5):576-578
A series of benzenesulfonylurea derivatives possessing a branched hydroxymethyl moiety as an ortho-substituent were synthesized and found to have interesting herbicidal activity under submerged paddy conditions. 相似文献
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Jablonkai I 《Pest management science》2003,59(4):443-450
The relationship between S- and N-alkylating reactivity and herbicidal activity within a series of chloroacetamides, including several commercial herbicides and newly synthesised analogues was studied. The S-alkylating reactivity of selected chloroacetamides, as well as those of atrazine and chlorfenprop-methyl, was determined by in vitro GSH conjugation at a ratio of GSH to alkylating agent of 25:1. A spectrophotometric reaction using 4-(4-nitrobenzyl)pyridine was used to characterise the N-alkylating reactivity of the chemicals. Our results indicate that a reduced level of N-alkylating reactivity correlates with an improved herbicidal efficacy at a practical rate. However, the phytoxicity of the molecules is not simply dependent on chemical reactivities, but strictly related to the molecular structure, indicating that lipophilicity, uptake, mobility and induction of detoxifying enzymes may also be decisive factors in the mode of action. 相似文献
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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
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Siddall TL Ouse DG Benko ZL Garvin GM Jackson JL McQuiston JM Ricks MJ Thibault TD Turner JA Vanheertum JC Weimer MR 《Pest management science》2002,58(12):1175-1186
A novel series of substituted 3-phenyl benzoylpyrazoles were prepared and tested as potential grass herbicides. The targeted materials were prepared by three newly developed synthetic routes, which allowed a comprehensive study of the SAR (structure-activity relationships) of this series. The best combination of grass weed activity (Avena fatua L, Setaria viridis (L) Beauv and Alopecurus myosuroides Huds) and wheat selectivity was obtained with an alkoxy group in the 4-position of the phenyl ring. Activity was further enhanced by the presence of tert-butyl on the pyrazole and a methyl group at the C-2 position of the benzoyl moiety. The alkoxy-substituted 3-phenylbenzoylpyrazoles are a novel class of herbicides with potential utility for control of important grass weeds in cereals. 相似文献
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为评价5-氧代三酮类化感物质AB5046A和AB5046B及其衍生物的除草活性,以均三酚为起始原料合成了天然化合物AB5046A和AB5046B,同时合成了13个2-脂肪酰基和2-芳香甲酰基衍生物,并采用小杯法和平皿法测定了它们及其衍生物对油菜和稗草的生物活性。结果表明:所建立的合成方法仅通过5步反应即可分别以36%和28%的较高收率合成AB5046A和AB5046B,包括:(1)均三酚通过部分氢化还原和酸性离子交换树脂以83%的产率转化为3-乙氧基-5羟基-环己烯酮;(2)通过对羟基氯甲基甲醚保护,以80%的产率得到酮,(3)经3 mol/L HCl去乙基,进一步在4-N,N-二甲基氨基吡啶(DMAP)/二环己基碳二亚胺(DCC)条件下与相应等量羧酸缩合,分别以77%和71%的产率得到二酮,(4)~(5)随后在三甲基碘硅烷/4A分子筛条件下反应,分别以83%和70%的产率完成AB5046A和AB5046B的合成。AB5046A和AB5046B及其衍生物具有明显的除草活性,油菜和稗草表现出白化和褪绿特征,其中在100 μg/mL浓度下,AB5046A和AB5046B对油菜的根长抑制率均为43.9%,对稗草的株高抑制率则为38.6%和53.2%。在合成的13个衍生物中,5-羟基保护的衍生物2-正辛酰基-3-羟基-5-氧甲氧基甲基-2-环己烯酮(TM-6)对油菜和稗草的抑制率分别达到70.2%和62.5%,除草活性较2个天然产物明显提高,可以作为除草剂先导结构进行优化。 相似文献
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四唑啉酮衍生物在医药、农药和材料领域具有广泛的研究和应用价值,特别是在除草活性方面。对两类四唑啉酮衍生物的研发过程、除草活性和代谢方面的研究进展进行了综述,对其发展趋势和应用前景进行了展望。 相似文献
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This paper reports the synthesis and the biological activity of substituted 6-alkyl-1,2,3,4-tetrahydro-1,1-dimethylnaphthalenes in which the substituents at the 5- and/or 7-position are varied with a multitide of functional groups. These compounds exhibited pre-emergent herbicidal activity which was a function of the electron-withdrawing ability and the size of the groups substituted at the 5- and/or 7-position. Nitro and/or nitrile groups at these positions tended to optimize activity. 相似文献
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Narihito Ogawa Ryoya Imaizumi Tatsuya Hirano Jun Suzuki 《Journal of Pesticide Science》2021,46(3):278
We investigated the synthesis and herbicidal activity of 23 toxoflavin analogs, 1a–w, in which aromatic rings (R) were introduced into the C-3 position. In paddy field conditions, 1k (R=2-CF3–C6H4) and 1w (R=2-thienyl) showed excellent herbicidal activity. Under upland field conditions, we found that toxoflavin analogs 1a (R=C6H5), 1n (R=2-CH3O–C6H4), and 1p (R=4-CH3O–C6H4) exhibited wide herbicidal spectrum against Echinochloa crus-galli (L) var. crus-galli (ECHCG), Chenopodium album, and Amaranthus viridis (AMAVI). The analog with the 2-fluoro group on benzene ring 1b also showed high herbicidal activity against both ECHCG and AMAVI. 相似文献
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为了寻找具有较高除草活性的异香豆素类化合物,设计合成了16个新型异香豆素噁二唑类化合物4a~4p,其结构均经核磁共振氢谱、碳谱及高分辨质谱确证。初步除草活性测定结果表明,部分目标化合物在500 mg/L下对马唐Digitaria sanguinalis L.和反枝苋Amaranthusretroflexus L.具有一定的除草活性,其中化合物4j(4-[5-(4-氯-苯基)-[1,2,4]二唑-3-基]-3-己基-6,7-二甲氧基异香豆素)的活性最好,对马唐和反枝苋的致死率分别为64%和62%。 相似文献
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设计合成了一系列结构新颖的嘧啶联吡唑甲酰胺类化合物5a~5o,其结构均经过1H NM R和MS分析确证。初步生物活性测试结果表明:在有效成分150 g/hm2剂量下苗后茎叶喷雾处理时,化合物(R)-N-[1-(4-氯苯基)乙基]-3-二氟甲基-1-(4,6-二甲氧基嘧啶-2-基)-1H-吡唑-4-甲酰胺(5c)、N-[1-(4-氯苯基)乙基]-1-(4,6-二甲氧基嘧啶-2-基)-N-甲基-3-三氟甲基-1H-吡唑-4-甲酰胺(5i)和N-[1-(4-氯苯基)乙基]-1-(4,6-二甲氧基嘧啶-2-基)-3-三氟甲基-1H-吡唑-4-甲酰胺(5k)对繁缕Stellaria media的抑制率高达90%以上;而同样剂量下苗前土壤喷雾处理时,化合物N-[1-(4-氯苯基)乙基]-3-二氟甲基-1-(4,6-二甲氧基嘧啶-2-基)-1H-吡唑-4-甲酰胺(5b)和5c对繁缕的抑制率达100%。该类结构化合物有望作为除草先导化合物进行开发。 相似文献
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Synthesis and herbicidal activity of novel heterocyclic protoporphyrinogen oxidase inhibitors 总被引:1,自引:0,他引:1
Meazza G Bettarini F La Porta P Piccardi P Signorini E Portoso D Fornara L 《Pest management science》2004,60(12):1178-1188
Protox inhibitors are applied as foliar sprays, thus causing very rapid cellular collapse and desiccation of many troublesome weeds in the presence of light. In many respects, they appear to be ideal herbicides, because they act rapidly and do not harm mammals under normal conditions. The main limitation to their widespread adoption is that few crops are naturally resistant to them. Crop tolerance has mainly been pursued with the synthesis of the cyclic imide classes containing 5- and 6-membered heterocycles, including pyrazole, pyridazine, 1,2,4-triazine, triazolinone and trifluoromethyluracil derivatives. Because of their structural novelties and biological performance, active investigations on heterocyclic protox inhibitors have been carried out in our laboratories and we have found 3-arylpyrroles to be a new class of light-activated, membrane-disrupting herbicides. They are active on both grass and broadleaf weeds at low rates. The synthesis and structure-activity relationships are presented. 相似文献
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丙炔氟草胺除草活性及对棉花的安全性 总被引:2,自引:3,他引:2
丙炔氟草胺是一种以原卟啉原氧化酶为作用标靶的N-苯基肽酰亚胺类除草剂。为探究其在棉花田的应用前景,通过温室盆栽法对丙炔氟草胺的杀草谱、除草活性及其对棉花的安全性进行了测定。结果表明:丙炔氟草胺对棉田常见阔叶杂草有较好防效,处理剂量为有效成分15 g/hm2时,对马齿苋Portulaca oleracea、反枝苋Amaranthus retroflexus、藜Chenopodium album、小藜Chenopodium serotinum和鳢肠Eclipta prostrata的鲜重防效均高于90%,对野油菜Rorippa indica、苣荬菜Sonchus arvensis、小飞蓬Conyza canadensis、龙葵Solanum nigrum、马唐Digitaria sanguinalis和牛筋草Eleusine indica等的鲜重防效高于80%;丙炔氟草胺对棉田4种常见阔叶杂草马齿苋、反枝苋、龙葵和藜的除草活性均显著高于二甲戊灵;丙炔氟草胺在鲁棉研28号与马齿苋、反枝苋、龙葵和藜之间的选择性指数依次为79.1、38.1、32.1和112.6,均显著高于二甲戊灵的12.0、9.9、5.8和9.2;鲁棉研37号、鑫秋4号与杂草间的选择性指数,与鲁棉研28号的相近。试验结果表明,丙炔氟草胺可作为棉田苗前防除阔叶杂草的候选药剂之一。 相似文献
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Janet E. Anderson Stephen Bell Wayne M. Best Peter F. Drygala Keith G. Watson Ian B. Bryan 《Pest management science》1996,46(2):131-138
A series of 1,4-benzoxazin-3-ones with a sulfonylurea group attached at either the 5 or 8 position have been synthesised and found to show moderate herbicidal activity. Similarly, a series of 1,4-benzothiazin-3-ones, including some of the related S-oxides and S-dioxides, with a sulfonylurea group linked at the 8 position, have been prepared and been found to be herbicidal. In both series of compounds many substituent variations were made but none of the compounds showed any useful crop selectivities. 相似文献