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1.
The effect of organotin compounds on the growth of Ceratocystis ulmi, the causative agent of Dutch elm disease, was studied in shake culture. Triphenyltin, (C6H5)3SnX, tricyclohexyltin, (C6H11)3SnX, and tributyltin, (C4H9)3SnX, compounds were all effective in the inhibition of C. ulmi in vitro. The anionic group, X, did not play a major role in the inhibitory activities of these compounds, suggesting that the species involved in the inhibition is R3Sn+ or the hydrated cation.  相似文献   

2.
Strains of Culex quinquefasciatus Say, selected with biopermethrin [(1R)-trans-permethrin] or with (1R)-cis-permethrin, were examined in the larval stage for crossresistance to 30 pyrethroids, DDT, dieldrin, temephos, propoxur, and two organotin compounds. The (1R)-trans-Permethrin-R strain [resistance factor (RF) = 4100-fold] and the (1R)-cis-Permethrin-R strain (RF= 450-fold) of C. quinquefasciutus were cross-resistant to all pyrethroids tested [RF= 12-fold for an allethrin isomer to about 6000-fold for (RS,RS)-fenvalerate] as well as to DDT (RF= about 2000-fold). However, they were not significantly Cross-resistant to dieldrin, temephos, propoxur, and the two organotin compounds. Changes in the alcohol moiety, structural isomerism, and susceptibility of the cyclopropane C-3 side chain to oxidative attack are important factors in determining the level of cross-resistance to various pyrethroids. Limited synergism of the pyrethroids by S,S,S-tributyl phosphorotrithioate and piperonyl butoxide (PB), and of DDT by chlorfenethol and PB, suggested that some non-metabolic mechanism, such as kdr, may be an important component of resistance to pyrethroids as well as to DDT in this mosquito.  相似文献   

3.
Ph3SnCl, Ph3SnAc (Brestan), Cy3SnOH (Plictran), and (Bu3Sn)2O (TBTO) markedly reduce the weight of the spleen and the gain in body weight of young mice feeding for 7 days on diets containing 260 μequiv organotin/kg diet. With mature mice feeding for 4 days on diets containing 780 μequiv organotin/kg, these compounds result in a loss in spleen weight and body weight and an alteration in the blood composition (reduction in lymphocytes and total leucocytes and an increase in erythrocytes, hemoglobin level, and hematocrit value). Four other organotins, [(PhCMe2CH2)3Sn]2O (Vendex), PhSnCl2, Ph2SnCl2, and Ph4Sn, are much less toxic based on these parameters. Poisoning by these dietary triorganotins was not related to cerebral edema or alterations in adrenal epinephrine level, liver nonprotein -SH groups, or the activity of digestive enzymes (intestine and stomach proteases and intestine amylase and invertase). The most sensitive indices of triorganotin toxicity appear to be those associated with changes in the lymphatic tissues and blood composition.  相似文献   

4.
The antifeedant effect of five organotin compounds (fentin acetate, fentin hydroxide, fentin chloride, cyhexatin and fenbutatin oxide) and of three other compounds known to possess antifeeding activity (guazatine triacetate, 4′-chloroacetophenone isobutyrylhydrazone and thiram) was investigated by feeding treated alfalfa to larvae of Boarmia selenaria. The three fentins and cyhexatin were highly active at 0.1 g litre?1, the order of activity at this concentration being fentin chloride > fentin hydroxide > fentin acetate ? cyhexatin, whereas the other compounds were practically inactive at either this or a somewhat higher concentration (0.5 g litre?1). Guazatine triacetate had a concentration-independent antifeedant effect at much higher concentrations (5–20 g litre?1).  相似文献   

5.
Forty new organofluorine compounds, containing phosphorus, have been synthesised as potential pesticides. The compounds include esters of O,O-dialkyl phosphoramidic acids of the type (RO)2P(O)NHAr; thioesters of O,O-dialkyl thiophosphoramidic acids of the type (RO)2P(S)NHAr; esters of O,O-dialkyl phosphonic acid of the type (RO)2P(O)Ar and esters of O,O-dialkyl thiophosphonic acid (RO)2P(S)OAr. All the compounds have been screened for their insecticidal activity against adult cockroaches (Periplanata americana) and a few show appreciable activity.  相似文献   

6.
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   

7.
基于结构拼接思想,设计合成了10个N-取代氨基香豆素类化合物,并测定了其抑菌及除草活性。6-硝基香豆素经Fe/NH4Cl还原得6-氨基香豆素,再与不同醛缩合得Schiff碱,最后经硼氢化钠还原制得10个N-取代氨基香豆素类化合物(4a~4J),其中9个未见文献报道,其结构均经红外光谱、核磁共振氢谱和质谱确认。抑菌活性测试结果表明,所有化合物对苹果腐烂病菌Valsa mali、葡萄白腐病菌Coniothyrium diplodiella、棉花枯萎病菌Fusarium oxysporium和柑橘炭疽病菌Citrusanthrax bacteria均有一定抑制作用,其中 4e 的抑菌活性最强,对苹果腐烂病菌和柑橘炭疽病菌的EC50值分别为7.53和12.93 mg/L,对其余2种植物病原菌的EC50值均小于25 mg/L;化合物 4f 次之,对苹果腐烂病菌和葡萄白腐病菌的EC50值均约为11 mg/L。除草活性测试结果表明,除 4f 外,所有目标化合物均有一定除草作用,其中 4c 的活性最强,100 mg/L下对反枝苋Amaranthus retroflexus种子根、茎生长的抑制率均为99%。  相似文献   

8.
For the first time in sterile nutrient media in the absence of the host plant, different forms and rates of nitrogen compounds were screened for their effect onS. hermonthica Benth. shoot development beyond seed germination. There was no shoot formation beyond the inoculation stages whenS. hermonthica germlings were grown in media devoid of nitrogen source. In culture media containing some nitrogen sources, healthy shoots were formed. Increasing concentrations of KNO3, NaNO3, Ca(NO3)2, Mg(NO3)2 and asparagine resulted in a significant increase inS. hermonthica shoot development. Inversely, increasing concentrations of (NH4)2SO4, NH4H2PO4, NH4Cl and urea led to increasing significant reduction ofS. hermonthica shoot development. The amino acids, glycine and asparagine supported reduced shoot development ofS. hermonthica, indicating that organic nitrogen cannot replace inorganic nitrogen forStriga growth. The ammonium nitrogen compounds, (NH4)2SO4 and NH4H2PO4, suppressed further shoot elongation and total dry weight of 20 and 40 days oldStriga hermonthica plants, in sterile culture media. The organic compounds urea, allylthiourea and thiourea had an effect similar to ammonium compounds. Arginine and glycine on the other hand did not suppress the further development of the parasite. The suppressive effect of nitrogen however, was greater when the parasite was 20 days old than when it was 40 days old. This work provides data to show that some nitrogen compounds reduce the severity ofS. hermonthica attack by direct suppression ofStriga growth and development at the post-germination stage and after shoots have been formed.  相似文献   

9.
Thirty-six new nitro-alcohol derivatives were synthesised. Tested in vitro against Helminthosporium sativum, the compounds had high antifungal activities; the EC50 values varied between 10?2 and 10?6 M , and for the majority of the compounds between 10?4 and 10?6 M . The EC50 values were calculated by probit analysis, except for the compounds with low activity, for which the values were estimated. Interesting relationships between the structure and antifungal action of the compounds were established.  相似文献   

10.
This work using purified recombinant human estrogen sulfotransferase (hSULT1E1) aimed to investigate the mechanism of the inhibition of estrogen sulfation by organotin compounds. Tributyltin (TBT) inhibited the sulfation of estrone (E1) and 17 β-estradiol (E2) by hSULT1E1 competitively, with IC50 values of, respectively, 3 and 12 μM. The sulfation of E1 and E2 was also inhibited competitively by triphenyltin (TPT), with IC50 of, respectively, 10 and 5 μM. These data strongly suggested that His107 residue might act as a ligand to establish a coordination bond with organotins at estrogen binding site in hSULT1E1. A more surprising finding was that TBT competed with 3′-phosphoadenosine 5′-phosphosulfate (PAPS), indicating that TBT may coordinate with certain amino acid residue such as Lys47 at the PAPS binding site of hSULT1E1. Taken together, these data provided clear evidence that TBT and TPT have a capacity to disrupt endocrine-mediated events by inhibiting hSULT1E1 involved in the metabolism of sex steroids.  相似文献   

11.
Fifty-three heterocyclic sulphonyl derivatives including eight sulphonamides, three sulphonyl azides, nine sulphonohydrazides and twenty sulphonohydrazones of substituted thiophenes, and a smaller range of analogous isoxazoles pryazoles and thiazoles, were tested as potential fungicides in a simple screening procedure against Mucor mucedo, Septoria nodorum, Trichoderma viride, Chaetomium globosum and Aspergillus niger. Several thiophene-2-sulphonyl based compounds exhibited a high level of antifungal activity at 100 mg litre?1 against the five test species, especially the mono-halogen-substituted sulphonamides and sulphonohydrazines, in which a single chlorine or bromine atom was substituted in the para position of an attached phenyl ring. The most active compound, against all five species of fungus was N-(4-chlorophenyl)-N-(trichloromethylthio) thiophene-2-sulphonamide which had average MIC50 and MIC100 values of 86 and 180 μmol respectively. (MIC50 and MIC100 values are, respectively, the concentrations required to inhibit fungal growth by 50% and to inhibit it totally.) In general, the isoxazole analogues of the thiophene-2-sulphonyl compounds exhibited a much lower fungitoxic activity, whilst the pyrazole and thiazole based compounds had little or no activity. Compared with the other results, the considerable activity shown by 4-[2′-(3,4-dichlorobenzylidene)hydrazinosulphonyl]thiophene-2-carboxylic acid was unexpected.  相似文献   

12.
为了寻求和开发新的基于天然产物的杀螨剂,在明确姜黄素具有杀螨活性,且其结构中的双羰基并非杀螨活性关键基团的基础上,设计并合成了15个姜黄素异噁唑和吡唑衍生物,其结构均经红外光谱、核磁共振氢谱和质谱分析确认。生物活性测定结果表明:几乎所有的目标化合物对朱砂叶螨Tetranychus cinnabarinus和柑橘全爪螨Panonychus citri均表现出了比先导化合物姜黄素更优异的触杀活性,其中化合物 4和11 的活性最为突出。处理48 h后,化合物 4 对朱砂叶螨和柑橘全爪螨的LC50值分别为333.0和156.0 mg/L,其毒力是姜黄素的6.35和4.56倍, 11 的LC50值分别为478.4和144.7 mg/L,毒力是姜黄素的4.42和4.92倍;相应地处理72 h后, 4 的LC50值分别为115.0和84.9 mg/L,其毒力是姜黄素的5.02和1.43倍, 11 的LC50值分别为91.0和68.7 mg/L,毒力是姜黄素的6.35和1.77倍。化合物 4和11 可作为进一步开发研究的具有杀螨活性的候选化合物。  相似文献   

13.
Variously substituted benzyl derivatives of chloronicotinyl insecticides were synthesized with a wide range of substituents including halogens, NO2, CN, CF3 and small alkyl and alkoxy groups at the ortho, meta and para positions, as well as multiple‐substituted benzyl analogues. Their binding activity to the α‐bungarotoxin binding site in housefly (Musca domestica) head membrane preparations was measured. Among the compounds tested, the activity of the meta‐CN derivative was the highest, being 20–100 times higher than those of imidacloprid, acetamiprid and nitenpyram. The synergized insecticidal activity against houseflies was also measured for selected compounds with the metabolic inhibitor, NIA16388 (propargyl propyl phenylphosphonate). For the nitromethylene analogues, including both benzyl and pyridylmethyl analogues, higher binding activity usually resulted in higher insecticidal activity. © 2000 Society of Chemical Industry  相似文献   

14.
The relationship between the hydrophobicity of certain herbicidal compounds and the bleaching pattern caused on radish cotyledons was investigated. Seed treatment with diphenylpyridones, as well as with established herbicides, produced three types of bleaching pattern according to their hydrophobicity. The less hydrophobic compounds caused complete bleaching of both cotyledons, but the compounds with more hydrophobicity caused only partial bleaching. The critical points for whole or partial bleaching were in the range of log Kow 4–5 (Kow: octanol/water partition coefficient), and these values were changed slightly with their chemical classes. Uptake of compounds into the seed coat took place rapidly; these compounds were then translocated slowly from the seed coat to the embryo, namely, radicle, abaxial surface of one cotyledon and marginal areas of both cotyledons. Application of these compounds to roots resulted in initial translocation to marginal areas of both cotyledons, with subsequent translocation to the middle area. It is believed that compounds taken up into the radicle were translocated to both cotyledons in a manner similar to that following application to roots. These effects following uptake by seeds can be used as a translaminal and lateral transport assay for bleaching herbicidal compounds in cotyledons.  相似文献   

15.
为了探索新型异齅唑啉类化合物作为杀菌剂候选化合物开发的潜力,本研究以廉价易得的芳香醛类化合物为原料制备了32个氯代肟类化合物,通过其与天然产物丁香酚的1,3-偶极环加成反应和后期官能团化反应,制备了35个异齅唑啉类化合物 ( D1 ~ D32 , E1 ~ E3 ),其中34个为新化合物。所有化合物的结构均经过液相色谱-电喷雾质谱 (LC-ESI-MS)、核磁共振氢谱 (1H NMR) 及元素分析确认。初步抑菌活性测试结果表明:多数目标化合物对油菜菌核病菌、水稻纹枯病菌、番茄早疫病菌和辣椒疫霉病菌具有较好的抑菌活性,其中化合物 D26 对油菜菌核病菌的活性最高,有效抑制中浓度 (EC50) 为14.3 mg/L,具有进一步研究的价值。  相似文献   

16.
N-Alkylated analogs (C1–C3) of an N-arylcarbamoylpyrazoline were prepared. The introduction of these alkyl groups completely changed the crystal structure in respect of the torsion angle of the amide C–N bond of the non-alkyl compound. The introduction of methyl and ethyl groups slightly, and that of an isopropyl group markedly, decreased insecticidal activity against American cockroaches and house flies. Conformational analyses of the compounds suggested that the insecticidally active conformer of this class of compounds is in the anti-position regarding the N′–C(=O) and N-aryl bonds in which the non-alkyl compound is energetically the most stable. The most stable conformers of the alkylated compounds are in the syn-position, and these compounds would interact with target sites in the less stable anti-form. © 1999 Society of Chemical Industry  相似文献   

17.
BACKGROUND: The development of environmentally friendly and novel structural pesticides is now an area of intense research in the agriculture field. Spirocyclic tetronic acids such as spiromesifen are typical compounds of this kind. In order to discover novel compounds with improved and broader-spectrum insecticidal activities, a series of spiromesifen derivatives were synthesised and bioassayed. RESULTS: The derivatives were identified by 1H NMR and MS. Preliminary bioassays demonstrated that some bioactivities of compounds 5a to 5u were better and had a broader spectrum than the lead compound spiromesifen. Moreover, these compounds showed better insecticidal activities against Mythimna sepatara and Aphis fabae than acaricidal activities against Tetranychus cinnabari. Furthermore, LC50 of 5s against Aphis fabae reached 1.09 mg L−1. At the same time, compounds 5g, 5i, 5k and 5r also warrant further study because of their superior bioactivities to spiromesifen. What is more, suitable carbon chain length in the 4-position ester and the log P value of these spiromesifen derivatives dramatically influenced their insecticidal activities. Butyric or pentanoic ester and a log P value of 4.0–6.0 may be preferred. CONCLUSION: The present work demonstrates that some spiromesifen derivatives can be used as potential lead compounds for developing novel insecticides and acaricides. Copyright © 2011 Society of Chemical Industry  相似文献   

18.
A pressure-chamber technique was used to study the root uptake and xylem translocation of some fungicides, herbicides and an insecticide from different chemical classes in detopped soybean roots. Physiological parameters such as K+ leakage from roots, K+ concentrations in the xylem sap, and protein and ATP levels in the root cells were measured so as to evaluate any potential damage of this technique to the root system. HPLC was used to quantify the compounds in the xylem sap. The pressure-chamber technique has proved useful to study the root uptake and translocation of pesticides, does not damage the root system, and allows one to obtain appreciable volumes of xylem sap that can be analysed directly by HPLC, thus avoiding dependence on the availability of radio-labelled compounds. The concentration of each pesticide in the xylem sap showed a steady-state kinetic profile. Non-linear regression analysis was used to calculate the steady-state concentration and the time required to achieve 50% of the steady-state concentration (TSSC50). TSSC50 was well correlated with log Kow; the more lipophilic the compound the more time was required to reach the steady-state concentration. The efficiency of translocation was assessed by the transpiration stream concentration factor (TSCF) and a non-linear relationship between TSCF and log Kow was observed. The highest TSCF values were measured for those compounds with log Kow values around 3, a lipophilicity value similar to that reported earlier in an analogous experiment with detopped soybean plants but slightly higher than that reported in earlier experiments with intact barley plants. Lower TSCF values were obtained with chemicals with log Kow values below as well as above 3. © 1997 SCI.  相似文献   

19.
Choline acetyltransferase (E.C.2.3.1.6) catalyses the synthesis of acetylcholine and is therefore a target for a new insecticide. We have prepared a variety of compounds, mainly choline analogues, as inhibitors of this enzyme. One of these, 2-isothiocyanatoethyltrimethylammonium iodide, has a Ki of 0.06 μM (Km for choline is 150 μM ) and is apparently the most powerful inhibitor known for this enzyme. Although some of our compounds are insecticidal we believe, on the basis of electrophysiological studies, that they act, not on choline acetyltransferase, but on the acetylcholine receptor of the insect.  相似文献   

20.
The eradicant activities of 24 nitrogen-containing preparations, comprising primary, secondary or tertiary amines, amine acetates, diamines, amine oxides or quaternary ammonium salts, were assessed in trials with potted dormant apple rootstocks, heavily infected with the powdery mildew fungus Podosphaera leucotricha. The surfactants consisted of mixtures in which C12/C14 or C16/C18 alkyl or alkenyl compounds predominated. Of the amine acetates (at 50g litre?1), only the formulation containing C12/C14 primary amine acctates was considered worthy of further evaluation. Some amine oxides and quaternary ammonium compounds (at 35 g litre?1) were good eradicants and were as effective as ‘PP222’ a (nonylphenol-ethoxylate mixture) which was included for comparison. All the compounds showing good activity contained one C12/C14 alkyl group whereas C16/C18 compounds, whether saturated or unsaturated, were relatively inactive. In a field trial, C12/C14 (dimethyl) amine oxide, C12/C14bis (2-hydroxyethyl) amine oxide, and C12/C14 amine acetate (35 g litre?1) greatly reduced the amount of primary mildew on trees that were previously heavily infected, but there were signs that the fruit yield was reduced.  相似文献   

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