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1.
Nitroguanidine derivatives with thiazol-5-ylmethyl moieties were prepared and their insecticidal activities against homopterous pests were tested. New synthetic routes for 2-chloro-5-chloromethylthiazole from 2,3-dichloro-1-propene and for substituted nitroguanidines from S-methyl-N-nitroisothiourea were established. Biological evaluation led to a novel insecticide (E)-1-(2-chlorothiazol-5-ylmethyl)-3-methyl-2-nitroguani dine (TI-435) which has a broad activity spectrum and is under development. ©1999 Society of Chemical Industry  相似文献   

2.
The molluscicidal activities of ten Baylis-Hillman adducts against Biomphalaria glabrata (Say) snails, the intermediate host of schistosomiasis, have been determined. Nine of these compounds showed significant molluscicidal activity against B. glabrata, falling below the threshold of 100 microg ml(-1) set for potential molluscicidal activity by the World Health Organisation. Among these compounds, 3-hydroxy-2-methylene-3-(4-nitrophenyl)propanenitrile had the highest activity, with LC(50) = 6.64 microg ml(-1).  相似文献   

3.
以(E)-2-[2'-(bromo-methyl)phenyl]3-甲氧基丙烯酸甲酯和2(1H)-喹啉酮类化合物为原料,通过醚化等反应,合成了11个新型含2(1H)-喹啉酮结构的甲氧基丙烯酸酯类化合物,其结构经红外、电喷雾串联质谱(ESI-MS)和核磁共振氢谱确证。初步生物活性测试结果表明:在100 mg/L质量浓度下,部分目标化合物对烟草赤星病菌Alternaria alternata等6种病原菌具有一定的抑菌活性,其中5a对水稻稻瘟病菌Pyricularia grisea的抑菌率达100%。  相似文献   

4.
New pyrethroids containing heterocyclic rings in the alcohol moieties were synthesised and their insecticidal activities were studied. Of these new pyrethroids, 3-benzylpyrrol-1-ylmethyl (1RS-cis, trans-3(2,2-dichlorovinyl)-2,2-dimethylcyclopropanecarboxylate was found to be the most effective, having higher activity than permethrin against Musca domestica by a topical application method. In addition, para-substituted analogues of the 3-benzylpyrrol-1-ylmethyl ester were also synthesised to study the substituent effects on insecticidal activities; the residual effects of these compounds against Blattella germanica were also examined.  相似文献   

5.
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   

6.
A series of 14 new 3-[4(3H)-quinazolinone-2-(yl)thiomethyl]-1,2,4-triazoles were prepared and characterized by elemental analyses, IR, [1H] NMR and mass spectral data. Four of the compounds showed insecticidal activity equivalent to that of malathion against the adult stage of the blow fly (Chrysomyia albiceps). However, their activity against the larval stages of this insect species was considerably weaker.  相似文献   

7.
A series of novel 2-(2,4,6-trisubstituted phenyl)-1,3,4-oxadiazolin-5-one derivatives and 3-(2,4,6-trichlorophenyl)pyrazolin-5-one derivatives were synthesized and evaluated for insecticidal activity. It was found that a moderately bulky alkyl group, such as a tert-butyl group, on the heterocyclic ring, and a trifluoromethyl group on the benzene ring were optimal substituents on the molecule. The oxygen atom in the oxadiazoline ring was essential for insecticidal activity. Of the compounds assayed, 4-tert-butyl-2-(2,6-dichloro-4-trifluoromethylphenyl)-1,3,4-oxadiazolin-5-one gave the highest activity against Nephtotettix cincticeps, with an LC50 value of 0.51 mg litre−1. © 1999 Society of Chemical Industry  相似文献   

8.
以氯虫苯甲酰胺和氟虫腈的结构为基础,通过活性亚结构拼接的方法,设计合成了24个新型含吡唑杂环邻氨基苯甲酰胺类化合物,其结构经1H NM R、IR及APCI-M S表征。初步生物活性测试结果表明:化合物5-溴-N-[4-氯-2-甲基-6-(甲氨基甲酰基)苯基]-1-1-[2,6-二氯-4-(三氟甲基)苯基]-4-三氟甲基亚磺酰基-1H-吡唑-3-甲酰胺(5k)和5-溴-N-[4-溴-2-甲基-6-(甲氨基甲酰基)苯基]-1-[2,6-二氯-4-(三氟甲基)苯基]-4-三氟甲基亚磺酰基-1H-吡唑-3-甲酰胺(5l)在500 mg/L下对朱砂叶螨Tetranychus cinnabarinus的致死率为100%,但在100 mg/L下其致死率则分别降至30%和50%。所得结果可为邻氨基苯甲酰胺类化合物构效关系研究提供参考。  相似文献   

9.
Bioassay data are reported for 12 organotin compounds, R3SnX, against the adult snail, Biomphalaria glabrata, an intermediate host of schistosomiasis. The relationship between the molluscicidal activity and the nature of the R and X groups in the organotin compounds is discussed, as well as the possible mode of toxic action of these compounds.  相似文献   

10.
Two fungal metabolites, aspyrone (3-(1,2-epoxypropyl)-5-hydroxy-6-methyl-5,6-dihydropyran-2-one) and asperlactone (3-(1,2-epoxypropyl)-5-(1-hydroxyethyl)-5-furan-2-one) were isolated from an Aspergillus ochraceus Wilhelm strain showing IGR activity against Tribolium castaneum (Herbst). Synthetic derivatives of aspyrone were produced using published methods. These derivatives together with aspyrone and asperlactone were tested for insect growth-regulating activity against T. castaneum, and for ovicidal activity against Nezara viridula L. Of the compounds tested asperlactone appeared to be the most active.  相似文献   

11.
The residues and metabolism of methidathion [S-(2, 3-dihydro-5-methoxy-2-oxo-1, 3, 4-thiadiazol-3-ylmethyl) O, O-dimethyl phosphorodithioate] and its secondary metabolites: demethyl-methidathion [S-(2, 3-dihydro-5-methoxy-2-oxo-1, 3, 4-thiadiazol-3-ylmethyl) O-methyl O-hydrogen phosphorodithioate] ( IV ), the sulphide (2,3-dihydro-5-methoxy-3-methylthiomethyl-1,3,4-thiadiazol-2-one) ( I ), tsulphoxide(2,3-dihydro-5-methoxy-3- methylsulphinylmethyl-1,3,4-thiadiazol-2-one) ( II ) and the sulphone (2,3-dihydro-5-methoxy-3-methylsulphonylmethyl-1,3,4-thiadiazol-2-one ( III ) were studied in laboratory-treated tomato fruit. The metabolites and residues of methidathion were determined for the applied doses of 1, 7 and 14 mg of methidathion kg?1 of fruit. Methidathion was metabolised extensively over a 14-day period. The amount of metabolites formed was a function of both the applied dose as well as the time after application. Major water-soluble metabolites were found to be IV and the cysteine conjugate S-(2,3-dihydro-5-methoxy-2-oxo-1,3,4-thiadiazol-3-ylmethyl)-L-cysteine ( VI ). The chloroform-soluble metabolites were identified as the oxygen analogue of methidathion [S-(2,3-dihydro-5-methoxy-2-oxo-1,3,4-thiadiazol-3-ylmethyl) O, O-dimethyl phosphorothioate] ( V ), the sulphoxide II , and the hydroxy compound 2,3-dihydro-3-hydroxymethyl-5-methoxy-1,3,4-thiadiazol-2-one. The oxygen analogue of methidathion ( V ) was found in small amounts, corresponding to <5% of the added methidathion. Demethyl-methidathion ( IV ) appeared to be a precursor in the formation of the cysteine conjugate VI . The sulphide I seemed to be more reactive in forming the cysteine conjugate than the sulphoxide II or the sulphone III .  相似文献   

12.
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   

13.
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   

14.
Six heterocyclic alkylating agents were synthesized and examined for activity against the oat stripe pathogenPyrenophora avenae on agar plates and against the barley powdery mildew fungusBlumeria graminis f.sp.hordei on barley seedlings. Radial growth ofP. avenae was not significantly affected by any of the compounds, but four of them,α,α-bis[4,7-bis(2-chloroethyl)-1,4,7-triazacyclononane]-para-xylene[3], 1,4,8,11-tetra(2-chloroethyl)-1,4,8,11-tetraazacyclotetradecane[4], 8,11-bis(2-chloroethyl)-1,4,8,11-tetraaza-5,7-oxocyclotetradecane[5] and 7,16-bis(2-chloroethyl-1,4,10,13-tetraoxa-7,16-diazaoctadecane[6], gave significant reductions in biomass ofP. avenae grown in liquid culture and in powdery mildew infection on barley when used at 25μM. Polyamine biosynthesis was examined by following the incorporation of labeled ornithine into polyamines inP. avenae. The four compounds3–6 which reduced mildew infection all reduced the flux of label through to the polyamines inP. avenae. Whether the reductions in mildew infection caused by these compounds is related to reduced formation of polyamines is not known and awaits investigation. http://www.phytoparasitica.org posting May 22, 2005.  相似文献   

15.
刘长春 《农药学学报》2015,17(1):97-100
以芳香硝基化合物、2-氯-5-吡啶甲醇和一氧化碳为原料,在Pd-Fe/Ti O2催化下进行羰基化反应,合成了11个新型氨基甲酸-2-氯吡啶-5-甲酯化合物,其结构经1H NM R和M S表征。初步抑菌活性测定结果表明:在50 mg/L下,大多数目标化合物对4种供试病原菌具有一定的抑制活性,其中化合物3f(4-甲氧基苯基氨基甲酸-2-氯吡啶-5-甲酯、3h(2,4-二氯苯基氨基甲酸-2-氯吡啶-5-甲酯)和3j(3,4-二氯苯基氨基甲酸-2-氯吡啶-5-甲酯)对小麦赤霉病菌Gibberella zeae的抑制率达77.3%以上,3f对苹果轮纹病菌Physalospora piricola的抑制率达82.5%,与对照药多菌灵接近;所有化合物在50 mg/L下对番茄灰霉病菌Botrytis cinerea的抑制活性均优于对照药多菌灵。  相似文献   

16.
以3-氨基-2-氯吡啶(1)为起始原料,经重氮化、叠氮化、环合和酰氯化反应,生成1-(2-氯吡啶-3-基)-5-甲基-1H-1,2,3-三唑-4-甲酰氯(5),(5)与取代苯胺反应,制得13个未见文献报道的吡啶联三唑类化合物,其结构通过 1H NMR和LC-MS表征。初步生物活性测定结果表明:在500 mg/L质量浓度下,所有目标化合物对粘虫 Mythimna separate 均有一定的杀虫活性,部分化合物致死率达100%;但在100 mg/L下,除化合物ZJ-7的致死率仍达100%外,其余化合物的活性明显降低,甚至无活性。  相似文献   

17.
N-Arylcarbamoylpyrazolines with various substituents at the para position of the carbamoyl benzene ring inhibited ATP-dependent Ca2+-uptake in synaptosomes prepared from the rat brain. The activity of these compounds was evaluated as log(1/I50), the reciprocal logarithm of half inhibitory concentration, I50 (m ), from the concentration–response curve for the inhibition of Ca2+-uptake. Among the compounds tested, methyl 3-(4-chlorophenyl)-4-methyl-1-[N-(4-trifluoromethylphenyl)carbamoyl]-2-pyrazoline-4-carboxylate was the most potent, the I50 value of which as 9·12×10−7 m . Variations in the activity in terms of log(1/I50) were quantitatively analysed using a substituent parameter, showing that the higher the electron-withdrawing effect of the substituent, the higher was the activity. The substituent effects were similar to those on insecticidal activity against the Americal cockroach. The higher the inhibitory activity against Ca2+ uptake, the higher seemed to be the insecticidal activity. Methyl(4S) - 3 - (4 - chlorophenyl) - 4 - methyl - 1 - [N - (4 - chlorophenyl)carbamoyl] - 2 - pyrazoline -4-carboxylate had higher inhibitory activity against Ca2+-uptake and higher in-secticidal activity than the R-isomer, but the difference was greater in theCa2+-uptake system.  相似文献   

18.
The synthesis of a series of mono- and disubstituted biphenyl-3-ylmethyl esters of 3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropanecarboxylic acid is described. The bioactivity of these compounds against Spodoptera eridania, Epilachna varivestis, Oncopeltus fasciatus, Acrythosiphon pisum and Tetranychus urticae is presented and discussed. Substitution of fluorine, chlorine and methyl groups in the 2-position of the biphenyl ring generally led to an increase in activity over the unsubstituted parent biphenyl ester. In addition, pyrethroid esters derived from these 2-substituted biphenyl-3-ylmethanols appeared to have a broader spectrum of activity than ‘classical’ pyrethroids. For example, the (1RS)-cis-3-(2,2-dichlorovinyl)-2, 2-dimethylcyclopro-panecarboxylic acid ester of 2-methylbiphenyl-3-ylmethanol was acaricidal, while maintaining a level of activity against other insects that was equal to or greater than cis-permethiin. Biological data on other esters of this novel alcohol are also presented.  相似文献   

19.
2-吡啶酰氨基环己烷基磺酰胺的合成与杀菌活性   总被引：2，自引：2，他引：0  
为了进一步研究环烷基磺酰胺类化合物的杀菌活性与构效关系,在前期工作基础上,对先导化合物进一步展开研究,合成了15个未见文献报道的2-吡啶酰氨基环己烷基磺酰胺类化合物。首先以2-氧代环己烷基磺酰胺为原料,经过还原胺化后得到2-氨基环己烷基磺酰胺;再与取代吡啶甲酰氯反应,得到目标化合物。分别通过菌丝生长速率法与黄瓜活体叶片法测定了目标化合物对番茄灰霉病菌Botrytis cinerea及其他5种植物病原菌的杀菌活性。结果表明:目标化合物对番茄灰霉病菌表现出较好的抑制活性,其中化合物V-8在离体条件下对番茄灰霉病菌的EC50值为1.41 mg/L,在500 mg/L下的活体防效为79.17%;此外,部分目标化合物在50 mg/L下,对水稻纹枯病菌、水稻稻瘟病菌、大豆根腐病菌、黄瓜绵腐病菌和辣椒疫霉的抑制率高于60%,其中,化合物V-7对黄瓜绵腐病菌的EC50值为2.7 mg/L,其活性高于对照药剂多菌灵（EC50值为4.4 mg/L）,有进一步研究的价值。  相似文献   

20.
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