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1.
3-Methyl-5-(acyl/alkyl)aminoisoxazole-4-thiocyanates were prepared by rhodanation of N-acyl/alkyl-3-methyl-5-isoxazolamines. These products were tested for antifungal activity against a series of phytopathogenic fungi of different taxonomic classes. Some of the compounds showed interesting in-vitro activity. The more active compound in the in-vitro test displayed a moderate preventive activity against Plasmopara viticola, Alternaria solani and Pyricularia recondita.  相似文献   

2.
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   

3.
A series of 1-aryl-1-(1H-1,2,4-triazol-1-yl)alkyl-1-silacyclopentanes has been synthesized by four-step reactions starting from 1-chloroalkyltrichlorosilane and tested for fungicidal activities in vitro for ten fungi and in vivo for four fungi occurring in rice, cucumber, tomato etc. Biological activities of the title compounds are strongly dependent upon the p-substituent on the phenyl group in the following order: F>Cl>Ph>OEt>H. Especially, 1-p-fluorophenyl-1-[1-(1H-1,2,4-triazol-1-yl)alkyl]-1-silacyclopentanes (alkyl=methyl or ethyl) showed significant fungicidal activity with a broad spectrum comparable to flusilazole in in-vivo assay. © 1998 SCI.  相似文献   

4.
The phenolic composition of olive roots and stems was studied by high performance liquid chromatography–mass spectrometry. The in vivo levels of the principal phenolic compounds found in olive plants infected by Phytophthora megasperma Drechsler and Cylindrocarpon destructans (Zinssm.) Scholten differed from the levels observed in non-infected plants. When the antifungal activity of these compounds against both fungi was studied in vitro, the most active were quercetin and luteolin aglycons, followed by rutin, oleuropein, p-coumaric acid, luteolin-7-glucoside, tyrosol and catechin. Microscopic study showed that these phenolic compounds affected the growth, morphology and ultrastructure of the fungi. Taken together, these findings suggest that the phenolic compounds present in olive plants play an active role in the protection against pathogen attack.  相似文献   

5.
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   

6.
通过N-烷基化反应合成了一系列新型含苯并咪唑的(S,S)-2,8-二氮杂双环[4.3.0]壬烷类衍生物,中间体化合物通过环化反应和酰化反应合成得到。所有新型化合物的结构均通过熔点测定、核磁共振氢谱和高分辨质谱确认。生物活性测试结果显示,目标化合物拥有中等的抗植物真菌活性,对东方粘虫Mythimna separata Walker和蚊幼虫Culex pipiens pallens具有中等到良好的杀虫活性。其中化合物6e和6f对油菜菌核Sclerotinia sclerotiorum、马铃薯晚疫Phytophthora infestans、小麦赤霉Fusarium graminearum等真菌具有良好的抗菌活性。化合物6e和6k在200mg/L下对东方粘虫的致死率为100%,化合物6h和6k在2mg/L下对蚊幼虫的致死率为75%。  相似文献   

7.
The paper reported the synthesis and antifungal properties and mechanism of action of a series of 2-substituted methylthio-5-(2,4-dichlorophenyl)-1,3,4-oxadiazole/thiadiazole and their corresponding sulfones. The preliminary biological test showed these compounds exhibit moderate to good antifungal activity. Particularly, the compounds 7g and 7c inhibited mycelia growth by approximately 50% (EC50) at 2.6–59.2 μg/mL and 17.2–54.4 μg/mL respectively against nine kinds of fungi. The extent of inhibition induced by 7c on Rhizoctonia solani and underlying mechanism of action were studied in vitro. Docking simulation was performed to position selected compounds into the active site of family 18 chitinases. Variation in d-GlcNAc content and chitinase activity indicated that 7c can act as chitinase inhibitor for controlling fungal pathogens in plants.  相似文献   

8.
A series of imidazole-1-carboxylates was prepared by reacting various alcohols with trichloromethyl chloroformate and imidazole or N,N'-carbonyl-diimidazole. They were tested for fungitoxic activity in vitro against two phytopathogenic fungi, Botrytis cinerea (grey mould) and Gibberella fujikuroi, and for preventive efficacy against grey mould on cucumber leaves. 1-(4-Substituted phenoxymethyl)-2,2-dimethylpropylimidazole-1-carboxylates showed excellent in-vitro activity against B. cinerea, and moderate activity against G. fujikuroi, and some of them also effectively controlled grey mould in vivo. A 1H-1,2,4-triazole derivative corresponding to an imidazole derivative did not have any activity, while a thiocarboxylate corresponding to an imidazole carboxylate showed excellent activity against both B. cinerea and G. fujikuroi.  相似文献   

9.
A series of N-(arylalkyl)maleimides was prepared for the reaction of maleic anhydride and N-(arylalkyl) amines, and their antimicrobial activities were examined. All compounds exhibited antibacterial activity against gram-positive bacteria such as Bacillus subtilis and Staphylococcus aureus. Almost all compounds exhibited antibacterial activity against the gram-negative bacterium, Escherichia coli, but were inactive against Pseudomonas aeruginosa. Activities against gram-positive bacteria were independent of the nature of the substituent on the benzene ring or the length of alkyl group, but that against gram-negative bacteria was influenced by these parameters. All N-(arylalkyl)maleimides showed activity against yeasts and mycelial fungi.  相似文献   

10.
BACKGROUND: The development of water-soluble nanodevices extends the potential use of compounds developed for other purposes (e.g. antifungal drugs or antibiotics) for applications in agriculture. For example, the broad-spectrum, water-insoluble, macrolide polyene antibiotic amphotericin B (AMB) could be used to inhibit phytopathogenic fungi. A new formulation embedding AMB in nanodisks (NDs) enhances antibiotic solubility and confers protection against environmental damage. In the present study, AMB-NDs were tested for efficacy against several phytopathogenic fungi in vitro and on infected living plants (chickpea and wheat). RESULTS: Compared with AMB in dimethylsulfoxide (DMSO), AMB-NDs increased the sensitivity of several fungal species to this antimycotic in vitro. Sensitivity varied with fungal species as well as with the forma specialis. Phytophthora cinnamomi, previously reported as insensitive to other polyene antimycotics, remained unaffected at the doses examined. Some effect against disease symptoms were obtained with AMB-NDs against fusarium wilt in chickpea, whereas the results were highly variable in wheat, depending on both the species and treatment regimen. CONCLUSION: The results confirm that formulation of AMB into ND increases its effectiveness against phytopathogenic fungi in vitro, opening the possibility for its use on infected plants in the field. Copyright © 2011 Society of Chemical Industry  相似文献   

11.
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   

12.
为研究拮抗菌株NF83-1的分类与生物学特性以及评价其生防能力,通过生理生化特征和16S rRNA基因序列分析对菌株NF83-1进行种属鉴定,以选择性培养基检测其分泌的多种胞外酶,以结晶紫染色法检测其生物膜的形成,采用室内平板对峙生长法测定其抑菌活性,室外盆栽法测定其对番茄立枯病的防效。结果表明,菌株NF83-1被鉴定为戴尔福特菌Delftia tsuruhatensis;菌株NF83-1能产生纤维素酶和嗜铁素,且能在管壁形成较厚的生物膜。菌株NF83-1对立枯丝核菌Rhizoctonia solani、甘蓝黑斑病菌Alternaria brassicae、油菜菌核病菌Sclerotinia sclerotiorum、梨胶孢炭疽病菌Colletotrichum gloeosporioides等病原真菌,梨火疫病菌Erwinia amylovora、番茄青枯病菌Ralstonia solanacearum、水稻细菌性条斑病菌Xanthomonas oryzae pv.oryzicola等革兰氏阴性病原细菌及革兰氏阳性细菌巨大芽胞杆菌Bacillus megaterium都具有明显的抑制作用;菌株NF83-1发酵液原液和100倍稀释液对番茄立枯病的防效分别为48.78%~57.69%和26.83%~36.54%。研究表明,菌株NF83-1是一株具有较好生防应用潜力的拮抗菌株。  相似文献   

13.
The relationship between the structures of a series of O, O-diaryl S-ethyl phosphorothioates and their activity against five fungi has been analysed using physico-chemical parameters of the molecules such as hydrophobic RM and electronic σ by means of multiple regression analysis. Both the hydrophobic and the electronic effects were found to have a significant contribution in determining the fungicidal activity of this series of compounds against all the test fungi.  相似文献   

14.
Nine diethyl chloroacetylanilidomethylphosphonates and ten diethyl α-(chloroacetylanilido)benzylphosphonates were prepared by N-chloroacetylation of the corresponding diethyl anilinomethyl- and anilinobenzylphosphonates. These were tested for antifungal activity against six phytopathogenic fungi. Most of the compounds showed moderate protective properties. No significant difference in activity was observed for compounds with an extra aryl ring substituent on the methylene group of the backbone. Compounds with electron-withdrawing substituents, especially chlorine, on the aniline site (R1) showed higher fungicidal activity than the other compounds with electron-donating groups as substituents.  相似文献   

15.
The GRAS compounds cinnamaldehyde (at 30 ppm), acetaldehyde (at 70 ppm), benzalde-hyde (at 50 ppm) and potassium metabisulphite (at 250 ppm) either completely inhibited or significantly reduced thein vitro mycelial growth ofGliocephalotrichum microchlamydosponim,Colletotrichum gloeosporioides andBotryodiplodia theobromae, the causative fungi of brown spot, anthracnose and stem end rot, respectively, of rambutan fruits,Nephelium lappaceum. The four compounds also significantly reduced the severity of all three diseases and the activity of pectic lyase and polygalacturonase enzymes secreted by the three fungi.  相似文献   

16.
以亚甲二氧基苯为起始原料,经过溴化、硫化、环化等反应合成了19个未见文献报道的6,7-亚甲二氧基硫代苯并二氢吡喃-4-酮衍生物,其结构均经核磁共振氢谱和质谱确认。初步抑菌活性测试结果表明,在50 mg/L下,目标化合物对供试7种植物病原菌均有不同程度的抑制作用,其中化合物5b、5i、5k和5l对马铃薯干腐病菌 Fusarium solani的抑制率均达75%以上,5h和5i对番茄灰霉病菌Botrytis cinerea的抑制率分别是67.7%和70.4%。  相似文献   

17.
The quantitative relationship between the structure of 2-methoxy-5-(substituted-phenyl)-1, 3, 2-oxazaphospholidine 2-sulfides (5-PMOS) and their insecticidal activity against the house fly. Musca domestica L., was analyzed using reported physicochemical parameters and regression analysis. The electronic nature of the substituent on the phenyl group of 5-PMOS has the most significant effect on the activity, followed by hydrophobic and steric effects; the optimum value of Σρ is zero and the more hydrophobic the substituents on the phenyl group, the higher the insecticidal activity. The plots of observed pLD50, values against calculated pLD50 values for compounds having substituents in the ortho-position deviated downwards from those of compounds having substituents at the meta and/or para positions. This ortho-effect, which reduces the insecticidal activity of compounds having substituents at the ortho-position, was expressed by a dummy parameter D, which has the value 2 for di-ortho-substituted derivatives, 1 for mono-ortho-substituted derivatives and zero for others. Thus, the highest activity was obtained for 2-methoxy-5-phenyl-1, 3, 2-oxazaphospholidine 2-sulfide, and the activity was decreased by the introduction of any substituents on the phenyl group.  相似文献   

18.
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   

19.
N-(芳基磺酰氨基乙基)-1,6-己内酰胺的合成及杀菌活性   总被引:1,自引:0,他引:1  
以环己酮为原料,合成了9个结构新颖的N-(芳基磺酰氨基乙基)-1,6-己内酰胺( 3 ),其结构均经IR、1H NMR、13C NMR和元素分析确证。初步的生物活性测定结果表明,部分化合物对供试的6种病原真菌具有一定的杀菌活性,其中 3a、3b、3d和3g 对番茄叶霉病菌的抑制活性与对照药剂百菌清相当,抑制率大于90%。  相似文献   

20.
Antifungal rhizobacteria were obtained from maize, barley and chicory using direct or indirect isolation procedures. Effective isolates were tested for broad-spectrum activity against a set of phytopathogenic fungi. Isolates with broad-spectrum activity were identified as Pseudomonas fluorescens, P. cepacia, Serratia liquefaciens, S. plymuthica and Bacillus sp. Broad-spectrum compounds produced by P. cepacia and Erwinia herbicola were characterized as pyrrolnitrin and herbicolin-like compounds respectively.  相似文献   

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