共查询到16条相似文献,搜索用时 10 毫秒
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In the course of optimization studies around diafenthiuron, the central aromatic nucleus linked directly to the thiourea unit was replaced by a pyridine moiety. A series of N-(pyrid-3-yl)thioureas, -isothioureas and -carbodiimides was synthesised and evaluated for acaricidal activity. The synthetic methodology used and the screening results against some spider mites (Tetranychus spp. and Panonychus ssp.) are discussed. 相似文献
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Yoshinori Yamanaka Masaru Moritomo Katsutoshi Fujii Toshinobu Tanaka Yasuhisa Fukuda Keiichiro Nishimura 《Pest management science》1999,55(9):896-902
A set of N-(4-difluoromethoxybenzyl)pyrimidinamines with various substituents at the 4- and 5-positions of the pyrimidine ring and at the benzyl position were prepared, and their fungicidal activities against wheat brown rust, Puccinia recondita, and barley powdery mildew, Erisiphe graminis, were measured. Variations in each of these activities were quantitatively analysed by the use of physicochemical substituent parameters and a regression analysis. Each of these activities was parabolically correlated with the steric bulkiness of the pyrimidine substituents and with the bulkiness or the hydrophobicity of the benzylic substituents. © 1999 Society of Chemical Industry 相似文献
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Hussein M. Ali Hany A. Sharaf Eldeen Mohamed S. Hikal 《Pesticide biochemistry and physiology》2005,83(1):58-65
The inhibitory effects of a recently introduced series of the titled compounds on insect and mammalian acetylcholinesterase (AChE) activity were examined, where the median inhibition concentration (I50) and the inhibition kinetic parameters, bimolecular inhibition rate constant (ki), affinity constant (Ka), and phosphorylation rate constant (kp), were determined for each compound. Results indicated that all examined dioxaphospholenes had less inhibitory effects on mammalian AChE than fenitrothion, a commercial pesticide with moderate mammalian toxicity. The highest selectivity was obtained with compounds containing glutamic and leucine moieties (2.70 and 2.18, respectively) while selectivity of fenitrothion was 0.93. The low inhibitory effects of the examined dioxaphospholenes on mammalian AChE were attributed to their low phosphorylation rates (kp < 2.2 min−1) compared to that of fenitrothion (kp = 4.84 min−1). QSAR equations indicated that the inhibition process is controlled mainly by both the phosphorylation rate (direct effect) and the affinity of compounds toward the enzyme (inverse effect). Although the compounds’ hydrophobicity had no effects on the inhibition process, it affects the compounds’ toxicity since it affects the ability of compounds to penetrate insects to reach the enzyme active site. 相似文献
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Hirokazu Osabe Yasuo Morishima Yukihisa Goto Toshio Fujita 《Pest management science》1992,35(2):187-200
Using a set of representative members selected from 4-pyridone-3-carboxanilides and ortho-chlorinated diphenyl ethers exhibiting light-dependent herbicidal activity, we examined the three-dimensional structure-activity relationships quantitatively. The most stable conformation of each compound, regarded as the ‘active conformation’, was determined by either semi-empirical or ab initio molecular orbital calculations. With a hypothesis defining a common substructural skeleton between the two different compound series. each molecule was superimposed. We first analysed the structure-activity relationship using an index for the substructure shape similarity according to the superimposed conformations. After finding the relevance of the hypothesis, we examined the three-dimensional structure-activity relationship using the comparative molecular field analysis procedure. The results suggested that the two different series of compounds have a common region of the receptor site. The variations in the light-dependent herbicidal potency were governed by hydrophobicty and three-dimensional steric and electronic field parameters of molecules participating in the transport process and the interaction with the receptor site. The result was consistent with that derived from our previous quantitative analysis with the use of free-energy-related substituent parameters and the traditional regression procedure for a large number of pyridone-carboxanilides. 相似文献
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为了探索天然产物Cedarmycins衍生物的结构与活性关系,以α-亚甲基-β-羟甲基-γ-丁内酯为起始原料,经过与不同取代的羧酸缩合,合成了19个新的(4-亚甲基-5-羰基-3-四氢呋喃基)-苯甲酸甲酯衍生物。杀菌活性测定结果表明,该类衍生物具有广谱的杀菌活性,尤其对水稻纹枯病菌Rhizoctonia solani和辣椒疫霉Phytophthora capsici显示出很强的杀菌活性,其中化合物2e(R=2,4-2Cl)对这2种病菌的EC50值约为1.6 mg/L。 相似文献
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Yukio Nezu Nobuhide Wada Fumitaka Yoshida Takeshige Miyazawa Tsutomu Shimizu Toshio Fujita 《Pest management science》1998,52(4):343-353
The activity of a number of O-(4,6-dimethoxypyrimidin-2-yl)salicylic acids and their thio analogs inhibiting acetolactate synthase (ALS) preparation was measured. The effects of substituents on the salicylic-benzene ring on the inhibitory activity were analyzed quantitatively with physicochemical substituent parameters. For 6-substituted (thio)salicylic acids, the activity was shown to vary parabolically with the ‘intramolecular’ steric parameter ( Es ). In addition, the higher steric dimension of substituents in terms of the STERIMOL width or length parameter lowered the activity. The field-inductive electron-withdrawing property of the 6-substituents in terms of the Swain–Lupton–Hansch F was favorable for the activity of salicylic acid series. In 5-substituted salicylic acids, the activity was increased by electron-donating substituents with smaller size. The relationships between ALS inhibitory and herbicidal activities were also analyzed with some weed species. Both pre- and post-emergence activities against barnyard grass, Echinochloa crus-galli, were linearly related to the ALS inhibitory activity after allowing for the hydrophobic factor that may contribute to the transport processes. Those against two broad-leaved weed species, Polygonum convolvulus and Abutilon theophrasti were linearly related to the in-vitro activity with no significant participation of the hydrophobic factor. © 1998 SCI 相似文献
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Lamberth C Cederbaum F Jeanguenat A Kempf HJ Zeller M Zeun R 《Pest management science》2006,62(5):446-451
Novel types of anti-oomycetic compounds have been designed and prepared. The synthetic approach to these mandelamides is outlined. Biological data demonstrate their high efficacy against important plant diseases such as tomato and potato late blight (Phytophthora infestans De Bary) and grape downy mildew (Plasmopara viticola Berliner & de Toni). Structure-activity relationship studies are discussed. The new development product mandipropamid is presented. 相似文献
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含1,3,4-噻二唑的吡啶联吡唑乙酰胺类化合物的合成及除草活性 总被引:1,自引:1,他引:0
以乙酰丙酮、溴乙酸乙酯和2,6-二氯吡啶为起始原料,经取代、肼基化、环合、水解、酸化及缩合等反应,得到9个未见文献报道的吡啶联吡唑乙酰基类化合物 B1~B9 。其结构均经核磁共振氢谱和质谱表征。初步生物活性测定表明:在150 g/hm2的处理剂量下,大部分目标化合物表现出一定的除草活性,其中化合物 B2、B3、B6 和 B8 对苘麻Abutilon theophrasti Medicus、反枝苋Amaranthus retroflexus和凹头苋Amaranthus lividus L.生长的抑制率接近100%。 相似文献
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1-(3-氯吡啶-2-基)-5-二氟甲基-1H-4-吡唑酰胺类化合物的合成及杀菌活性 总被引:1,自引:0,他引:1
以2,3-二氯吡啶(1)为起始原料,经肼基化、环合、水解和酰氯化反应,生成1-(3-氯-2-吡啶)-5-二氟甲基-1H-吡唑-4-甲酰氯(6),(6)与取代基苯胺(7) 反应,制得13个未见文献报道的1-吡啶基吡唑酰胺类目标化合物。利用核磁共振氢谱、质谱(LC-MS)和元素分析对目标化合物的结构进行了表征。初步杀菌活性测定结果表明,在 50 mg/L下,大部分目标化合物对瓜类炭疽病菌Gibberella zeae、瓜类灰霉病菌Botrytis cinerea和水稻纹枯病菌Rhizoctonia solani的抑制活性均不高,仅ZJ-10对瓜类灰霉病菌的抑制率达76.03%。 相似文献
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IN TAEK HWANG HYOUNG RAE KIM JUNG SUB CHOI DONG JU JEON KYUNG SIK HONG JONG HWAN SONG KWANG YUN CHO 《Weed Biology and Management》2006,6(2):102-106
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
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Novel analogues of mandipropamid have been designed and prepared. The synthetic approach to these stretched and heterocyclic mandelamides is outlined. Biological data demonstrate their high efficacy against important plant diseases like tomato and potato late blight (Phytophthora infestans De Bary) and grape downy mildew (Plasmopara viticola Berliner & de Toni). Structure-activity relationship studies are discussed. 相似文献
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Functionalization of a nanostructured hydroxyapatite with Cu(II) compounds as a pesticide: in situ transmission electron microscopy and environmental scanning electron microscopy observations of treated Vitis vinifera L. leaves 下载免费PDF全文
Enrico Battiston Maria C Salvatici Alessandro Lavacchi Antonietta Gatti Stefano Di Marco Laura Mugnai 《Pest management science》2018,74(8):1903-1915