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1.
为寻找具有优异生物活性的氨基甲酸酯类化合物,根据活性亚结构拼接原理,将取代异 NFDA1 唑和肟醚基团引入多菌灵结构中,以取代苯甲醛 (1) 和2-氯苄胺(3) 为起始原料,经多步反应设计合成了10个未见文献报道的含肟醚并取代异 NFDA1 唑的氨基甲酸酯类化合物,其结构经 1H NMR 和 MS 确证。初步生物活性测定结果表明,部分目标化合物不仅具有一定的杀菌活性,同时还具有较好的除草活性。其中,活体盆栽试验结果表明,化合物11b对黄瓜霜霉病Pseudoperonospora cubensis 的相对防效为90%,对黄瓜白粉病Sphaerotheca fuliginea 的相对防效达95%,低于对照药剂多菌灵;除草活性皿测法表明,化合物11c和11j 200 mg/L下对靶标作物的根、茎抑制率均达80%以上,与对照药剂异丙酯草醚活性相当。盆栽法表明,150 g/hm2下,化合物11c和11j对繁缕Stellaria media苗前和苗后的抑制率均在70%以上,低于异丙酯草醚。此类化合物的构效关系有待进一步研究。 相似文献
2.
A series of novel oxime ether β-methoxyacrylates have shown good fungicidal activity against a number of fungal pathogens. These were designed by introducing a one- or two-atom spacer group adjacent to the oxime ether group. Best fungicidal activity was obtained when an amino spacer group was used. ©1999 Society of Chemical Industry 相似文献
3.
Hauk Solli Hans Berg Madsen Preben L. Hoist Per D. Klemmensen 《Pest management science》1976,7(5):503-511
Pyridyl terpenoid ethers have outstanding juvenile hormone activity in Tenebrio molitor compared with their phenyl analogues (6,7-epoxy-3,7-dimethyloct-2-enyl 6-ethyl-3-pyridyl ether and 7-ethoxy-3,7-dimethyloct-2-enyl 6-ethyl-3-pyridyl ether are active at 100 pg/larva). The compounds were also active in Galteria mellonella and Culex pipiens. 相似文献
4.
为寻求具有较高生物活性的农药新品种,以杀螨剂pyflubumide为先导,在其母体结构中引入肟酯和二芳基醚结构,设计并合成了7个未见文献报道的1H-吡唑-4-肟酯乙酰胺类化合物,其结构均经核磁共振氢谱、质谱和元素分析确证。初步生物活性测试结果表明,在500 mg/L质量浓度下,所有目标化合物对朱砂叶螨Tetranychus cinnabarinus均有较强的杀灭作用,大部分化合物对其的致死率达100%,但药效低于对照药剂阿维菌素和炔螨特。 相似文献
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6.
A series of novel 2-methylthio-3'/4'-substituted acetophenone oxime O-ethers were synthesized by the reaction of the corresponding acetophenone oximes with halides of pyrethroid alcohols in the presence of sodium hydroxide and phase-transfer catalysis or with triethyl quaternary ammonium salts of halides of pyrethroid alcohols in the presence of sodium hydroxide. These compounds showed notable insecticidal activity against Homopteran and Lepidopteran pests. 2-Methylthio-4'-fluoroacetophenone oxime O-[(2-methylbiphenyl-3-yl)methyl] ether was more effective than the commercial insecticides chlorfenapyr and fenvalerate. 相似文献
7.
Eiichi Kuwano Motohisa Shimizu Kenshi Shimazu Satoshi Nakazawa Koichi Suzuki 《Pest management science》1998,52(3):251-257
A new series of 5-(substituted phenoxy)pentyl 3-pyridyl ethers induced precocious metamorphosis in larvae of the silkworm, Bombyx mori. Both 2- and 4-pyridyl ethers were inactive, indicating that the 3-pyridine moiety was essential for the activity. Octyl, dodecyl and farnesyl 3-pyridyl ethers had no activity. Among the compounds tested so far, 5-(4-propylphenoxy)pentyl 3-pyridyl ether showed the highest activity. The activity fell off with increasing or decreasing length of the carbon chain between two oxygen atoms. Introduction of a methyl group at the 6 position of the pyridine ring completely eliminated the activity. Precocious metamorphosis induced by 3-pyridyl ethers was fully reversible by a simultaneous application of a small amount of tebufenozide, an ecdysteroid agonist, or methoprene, a JH agonist. © 1998 SCI. 相似文献
8.
Aiping Liu Xiaoguang Wang Can Chen Hui Pei Chunhui Mao Yongjiang Wang Haijun He Lu Huang Xinping Liu Zhibin Hu Xiaoming Ou Mingzhi Huang Jianren Yao 《Pest management science》2009,65(3):229-234
BACKGROUND: Although more than ten strobilurin analogues have been commercialized since 1996 as fungicides, only one was available as an acaricide as of 2003. To search for novel strobilurin analogues with unique biological activities, a synthetic screening programme was carried out. RESULTS: Syntheses of compounds analogous to the commercialized fungicide metominostrobin and the acaricide fluacrypyrim led to the discovery of a lead compound, (E)‐2‐{2‐[[3,5‐bis(trifluoromethyl)phenoxy]methyl]phenyl}‐2‐(methoxyimino)‐N‐methylacetamide (3b), that showed moderate acaricidal activity against Tetranychus urticae Koch. Compound 3b has a 3,5‐(CF3)2‐phenoxymethyl group instead of the unsubstituted phenoxy substituent in metominostrobin. Optimization of compound 3b was achieved by introducing an oxime ether bridge along with an alkylthio(alkyl) branch in place of the oxymethylene chain between two aromatic moieties, as well as by replacing the methoxyiminoacetamide group with a methoxyacrylate structure, leading to (E)‐ methyl 2‐{2‐[[[(Z)[1‐(3,5‐bis(trifluoromethyl)phenyl)‐2‐methylthioethylidene]amino]oxy] methyl]phenyl}‐3‐methoxyacrylate (6c) and (E)‐ methyl 2‐{2‐[[[(Z)[1‐(3,5‐bis(trifluoromethyl)phenyl)‐1‐methylthiomethylidene]amino]oxy]methyl]phenyl}‐3‐methoxyacrylate (9a, HNPC‐A3066). CONCLUSION: The above two compounds (6c, 9a) were shown to exhibit potent acaricidal and fungicidal activity. Compound 9a (HNPC‐A3066) also exhibits larvicidal and ovicidal activities against various acarids. The acaricidal potency is comparable with those of commercial acaricides such as fluacrypyrim, tebufenpyrad and chlorfenapyr. Copyright © 2008 Society of Chemical Industry 相似文献
9.
以芳氧吡啶乙酮分子插件为基础，设计合成了一系列芳氧吡啶乙酮肟醚类化合物，其结构经核磁共振氢谱、碳谱及高分辨质谱等确证。初步杀虫活性测定结果表明，该系列化合物对棉蚜 Aphis gossypii (Glover) 具有较好的杀虫活性，其中化合物 5a 和 6i 在50 μg/mL下对棉蚜的致死率分别为76.8%和70.1%，具有作为先导化合物进一步研究的价值；但其对小菜蛾的杀虫活性较差，在100 μg/mL下的致死率普遍低于30%。该系列化合物主要体现出了新烟碱类化合物的活性特征，为进一步研究其构效关系提供了新思路。 相似文献
10.
Michael J. Bull J. Hugh Davies Robert J. G. Searle Arthur C. Henry 《Pest management science》1980,11(2):249-256
The alkyl phenyl ketone oxime O-benzyl ethers are a new group of insecticidal compounds. Although they lack the ester linkage, they resemble the pyrethroids in general, and the esters of 2-phenylalkanoic acids, in particular fenvalerate, because they show similar physiological effects on isolated nerve preparations and on whole insects; they also show a similar pattern of change of biological activity in response to structural change. The compounds may exist as two geometric isomers, of which only the (E) series shows significant biological activity; this observation appears to have some bearing on the relationship between conformation and activity in the pyrethroid series as a whole. 相似文献
11.
Michael Elliott Richard L. Elliott Norman F. Janes Bhupinder P. S. Khambay David A. Pulman 《Pest management science》1986,17(6):691-700
Over 100 benzyl esters of pyrethroidal acids were synthesised and tested for insecticidal activity to establish detailed structure–activity relationships in compounds with side-chains similar to those in the natural pyrethrins. Alkenyl, and corresponding alkynyl, side-chains were effective, both at the 3- and 4-positions, as were side-chains with extended substitution in either E or Z forms. A cyano group at the α-position increases activity if the side-chain is at C-3, but lowers it drastically if the substituent is at C-4. Similarly, methyl groups at C-2 and/or C-6 may increase activity whether the unsaturated side-chain is at C-3 or C-4, but only in the absence of an α-cyano group. 相似文献
12.
A series of 2-(1-alkenyl)-3-hydroxy-1,4-naphthoquinones has been prepared and their toxicities assessed against Musca domestica. By comparison with analogous compounds having saturated 2-alkyl substituents, or unsaturated substituents with an unconjugated double bond (e.g. lapachol), it was demonstrated that the α-unsaturation of the substituent is responsible for a significant increase in the toxicity. The effect of the compounds against several other insect species and Tetranychus urticae follows completely different patterns. 相似文献
13.
Glynn Mitchell Eric D Clarke Stuart M Ridley Kevin J Gillen Shaheen K Vohra Daren T Greenhow 《Pest management science》2000,56(2):127-132
Derivatives of 2‐ethyl‐1,3,4(2H)‐isoquinolinetrione in which the 4‐keto group has been modified to (Z)‐oxime, (E)‐ and (Z)‐O‐methyl oxime, (Z)‐N,N‐dimethyl hydrazone, cyano‐imine and dicyanomethylene moieties have been prepared and evaluated as redox mediator herbicides. All of the compounds have the free‐radical properties required to function as redox mediators, as determined by cyclic voltammetry, though only the O‐methyl oximes, the N,N‐dimethyl hydrazone and the cyano‐imine have reduction potentials in the range required to stimulate the light‐dependent consumption of oxygen at photosystem I in isolated chloroplasts. The O‐methyl oximes and the cyano‐imine are fast‐acting post‐emergence herbicides, producing symptoms of rapid desiccation; the (E)‐O‐methyl oxime is the most active herbicide, being somewhat more potent than the parent isoquinolinetrione. Hydrolysis studies indicate that it is unlikely that any compound generates the parent isoquinolinetrione in vivo. Attempts to explain differences between in vitro and in vivo activities using hydrolytic stabilities and physical properties were unsuccessful, and it was concluded that these factors probably play a less significant role in moderating the herbicidal activity of isoquinolinetrione derivatives than originally thought. © 2000 Society of Chemical Industry 相似文献
14.
Manjree Agarwal Suresh Walia Swaran Dhingra Bhupinder P
S Khambay 《Pest management science》2001,57(3):289-300
Fresh rhizomes of Zingiber officinale (ginger), when subjected to steam distillation, yielded ginger oil in which curcumene was found to be the major constituent. The thermally labile zingiberene‐rich fraction was obtained from its diethyl ether extract. Column chromatography of ginger oleoresin furnished a fraction from which [6]‐gingerol was obtained by preparative TLC. Naturally occurring [6]‐dehydroshogaol was synthesised following condensation of dehydrozingerone with hexanal, whereas zingerone and 3‐hydroxy‐1‐(4‐hydroxy‐3‐methoxyphenyl)butane were obtained by hydrogenation of dehydrozingerone with 10% Pd/C. The structures of the compounds were established by 1H NMR, 13C NMR and mass (EI‐MS and ES‐MS) spectral analysis. The test compounds exhibited moderate insect growth regulatory (IGR) and antifeedant activity against Spilosoma obliqua, and significant antifungal activity against Rhizoctonia solani. Among the various compounds, [6]‐dehydroshogaol exhibited maximum IGR activity (EC50 3.55 mg ml ?1) while dehydrozingerone imparted maximum antifungal activity (EC50 86.49 mg litre?1). © 2001 Society of Chemical Industry 相似文献
15.
The relative potency to target and nontarget insects of ester pyrethroids and the analogous oxime ethers, and the degree of synergism of the esters with tributyl phosphorotrithioate, provide a useful guide to the importance of esterase detoxification in species specificity. These criteria indicate that esterase detoxification is a more important component of pyrethroid tolerance in Chrysopa carnea and Cryptolaemus montrouzieri larvae than in Exochomus flavipis larvae and Musca domestica adults. Studies with 3-phenoxybenzyl 2-(4-chlorophenyl)-2-cyclopropylacetate and the corresponding 2,3,4,5,6-pentafluorobenzyl ester, their oxime ether analogs, and permethrin and its thiol ester and amide analogs provide evidence that the high insecticidal activity of some ester and E-oxime ether pyrethroids, relative to that of the corresponding thiol ester and amide, is more closely associated with the dipole moment and polarizability of the central linkage and its resistance to esterase detoxification than with bond lengths or lipophilicities conferred by a specific linkage. Pentafluorobenzyl tetramethylcyclopropanecarboxylate is very effective in the vapor state for house fly control. 相似文献
16.
1-甲基-3-二氟甲基吡唑酰胺类化合物的合成及抑菌活性 总被引：1，自引：1，他引：0
以1-甲基-3-二氟甲基吡唑-4-甲酸为原料,经过1-甲基-3-二氟甲基吡唑-4-甲酰氯与相应的氨基苯并杂环类、芳胺类化合物反应,得到了14个未见文献报道的吡唑-4-甲酰胺类化合物(6a~6g、7a~7g),其结构均通过1H NMR、MS和IR表征。抑菌活性测试结果表明,在100 mg/L下,目标化合物对供试植物病原菌均有不同程度的抑制作用,其中7a~7g的抑菌活性较高,部分对苹果炭疽病菌的抑制率在90%以上。 相似文献
17.
Andrew W. Farnham Anderson Ifill Norman F. Janes Tariq Javed Bhupinder P. S. Khambay 《Pest management science》1990,28(1):25-34
New routes to the title compounds, involving improved conditions for the cyclopropanation, and a new method of constructing the central three-carbon unit (based on the coupling of a Grignard reagent with an allylic acetate) give access to products for which the previously reported route was not satisfactory. For the new route, a synthesis of 5-bromo-2-fluoro-diphenyl ether was developed. Previously deduced relationships between structure and insecticidal activity apply for the new compounds: alkenes are generally more active than corresponding alkanes; substitution at the 3- or 4-position (but not the 2-) of the 1-aryl group can enhance activity. In addition, some fluorine-containing substituents lead to high activity. 相似文献
18.
Anna Arnoldi Eliseo Betto Lucia Ceresa Gandolfina Farina Attilio Formigoni Remo Galli Leonardo Scaglioni 《Pest management science》1983,14(6):576-586
A series of 1-(3-pyridyl)-1-substituted-but-3-yn-1-ols and some related compounds were synthesised and tested for antifungal activity against eight phytopathogenic fungi of different taxonomic classes. High activity was shown in particular against Sphaerotheca fuliginea on Cucumis sativus. The compounds containing aromatic substituents gave the best results, not only in protectant but also in systemic and eradicant tests. The quantitative structure-activity relationship suggests that steric effects play an important role in determining fungicidal activity. 相似文献
19.
为探索新的农药先导化合物,经取代苯基呋喃甲酰氯与5-肼基-3(2H)哒嗪酮反应,得到15个未见文献报道的含呋喃环3(2H)哒嗪酮类化合物,其结构均通过了红外光谱、核磁共振氢谱和元素分析确认。初步生物活性测定结果表明,目标化合物具有良好的杀菌活性,但杀虫活性较弱。其中化合物3k在50 mg/L时对灰霉病菌的抑制率为86.29%±1.51%,与对照药剂腐霉利相当。初步的构效关系研究结果显示,苯环上取代基的种类和位置对杀菌活性有重要影响。 相似文献
20.
A number of quinazolin-4(3H)-one carbothioamides, pyrazoles, pyrazolones and tetrazole derivatives have been synthesised by the reaction of 2-hydrazino-3-(4-substituted phenyl)-quinazolin-4(3H)-ones with the appropriate aryl isothiocyanate, acetyl acetone, ethylacetoacetate and nitrous acid. All the compounds were tested in vitro for antibacterial, insecticidal and antifungal activity and found to have some activity. 相似文献