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1.
Seven 6-alkyl-3-n-butyl-7-hydroxy-4-methylcoumarins and three other related substituted coumarins were synthesised, characterised and tested for their toxicity towards mycelial growth of seven phytopathogenic fungi in culture. Rhizoctonia solani, Alternaria alternate, and Drechslera oryzae exhibited maximum sensitivity to these compounds whereas Pythium aphanidermatum, Colletotrichum falcatum, Fusarium solani and Macro-phomina phaseolina were less sensitive. The 6-n-butyl and 6-n-pentyl derivatives possessed strongest toxicity towards all fungi except C. falcatum but the corresponding 6-n-propyl derivative was inhibitory to only D. oryzae and A. alternata.  相似文献   

2.
A series of substituted 4-methylcoumarins was synthesised and the members tested for their toxicity towards mycelial growth of seven phytopathogenic fungi in culture. Rhizoctonia solani, Alternaria alternata and Fusarium solani exhibited maximum sensitivity to these compounds whereas Pythium aphanidermatum, Colletotrichum falcatum, Drechslera oryzae and Macrophomina phaseolina were relatively less sensitive. 6-Ethyl-3-n- propyl-7-hydroxy4-methylcoumarin ( I ) was relatively toxic towards all fungi except C. falcatum, P. aphanidermatum and M. phaseolina. The 6-n-butyl ( III ) and 6-(1, 1, 3, 3-tetramethylbutyl) ( VI ) derivatives were highly toxic to R. solani with EC50, values of lμg ml?1.  相似文献   

3.
Twelve 4-(substituted phenoxy)methyl-6-methyl coumarins were synthesised by the condensation of 4-chloromethyl-6-methyl coumarin with various phenols in the presence of potassium carbonate in dry acetone. The compounds were tested for their toxicity towards the mycelial growth of seven plant pathogenic fungi. Among the tested fungi, Pythium aphanidermatum, Colletotrichum falcatum, Drechslera oryzae, Alternaria alternata and Fusarium solani exhibited maximum sensitivity whereas Macrophomina phaseolina and Rhizoctonia solani were least sensitive to the test compounds. The 4-(4-tert-butylphenoxy)methyl and 4-(4-nitrophenoxy)methyl analogues possessed greatest toxicity towards the majority of the tested fungi.  相似文献   

4.
Relationships between their activities as blast control agents, and their abilities to inhibit mycelial melanisation on a nutrient agar, are described for 103 substituted benzothiazol-2(3H)-ones, benzoxazol-2(3H)-ones, indolin-2-ones, quinolin-2(1H)-ones, 1,2,3,4-tetrahydroquinolin-2-ones, benzo-1,4-thiazin-3(2H)-ones and benz-1,4-oxazin-3(2H)-ones, and some corresponding thiones. Several compounds in the respective series had a high protective activity and an antimelanisation activity against the blast fungus Pyricularia oryzae; furthermore, there was a good correlation in both of these activities, indicating that these compounds belong to the group of melanin biosynthesis inhibitors. Structural similarities of these compounds can be identified as follows: (a) having a benzo-bicyclic ring system; (b) containing a nitrogen atom in one ring at a position alpha to the benzene ring system; and (c) substitution, at the ring nitrogen atom, at the peri position in the aromatic ring relative to the nitrogen atom, and at the position alpha to the nitrogen atom in the ring system, with a double bond such as in carbonyl and thiocarbonyl groups. Among the compounds that have been proposed as melanin biosynthesis inhibitors, the chemical structures of tricyclazole, pyroquilon, 4,5-dihydro-4-methyltetrazolo[1,5-a]quinazolin-5-one (PP-389), [1,2,4]-triazolo[4,3-a]quinoline and 1-methylquinolin-2(1H)-one exhibit the structural similarities described above; however, 4,5,6,7-tetrachlorophthalide, 2,3,4,5,6-pentachlorobenzyl alcohol and N-substituted-2,3,4,5-tetrachloro-6-(hydroxymethyl)benzamides do not have such similarities in their chemical structures.  相似文献   

5.
The hydrolysis of 3, 4-dihydroprecocene I 3, 4-epoxide (3, 4-dihydro-7-methoxy-2, 2-dimethyl-3, 4-epoxy-2H-benzo[b]pyran), the putative ultimate cytotoxin of the insect growth regulator precocene I (7-methoxy-2, 2-dimethyl-2H-benzo[b]pyran), has been studied and found to exhibit first-order kinetics [k = 0.17 s?1 in 10 mm-phosphate buffer pH 7.0, containing 1, 4-dioxane (1 + 1 by volume), ionic strength 0.1]. Plots of log k versus pH, and k versus buffer concentration, suggest that the reaction is subject to both specific and general acid catalysis. High-performance liquid chromatography showed the reaction products to be predominantly the corresponding stereoisomeric diols (3, 4-dihydro-7-methoxy-2, 2-dimethyl-2H-benzo[b]pyran-3, 4-diol), the trans : cis ratio of which varied from 1.8: 1 to 2.2: 1 but was constant over the pH range 6-8, at a given buffer concentration. The results indicate that acid-catalysed hydration of 3, 4-dihydroprecocene I 3, 4-epoxide is an SN1 reaction, involving a trigonally hybridised carbocation at C4, even at physiological pH. Similar studies on 3, 4-dihydroiso-precocene I 3, 4-epoxide (3, 4-dihydro-6-methoxy-2, 2-dimethyl-3, 4-epoxy-2H-benzo-[b]pyran), a biologically inactive isomer of 3, 4-dihydroprecocene I 3, 4-epoxide suggest that an SNI mechanism also contributes to its hydrolysis, but the rate constant is 4000 times lower than that for 3, 4-dihydroprecocene I 3, 4-epoxide. Knowledge of the reactivity and mechanism of reaction of such compounds forms an important part of the basis for rational prediction of biological activity in precocene analogues, and hence their possible use as pest control agents.  相似文献   

6.
Photo-induced fungitoxicity was observed in Alternaria alternata, Aspergillus niger, Cladosporium variabile, Colletotrichum sp., Rhizopus nigricans, Pythium aphanidermatum, and Saprolegnia sp., elicited by 5-(but-3-en-l-ynyl)-2,2′-bithienyl, 2,2′: 5′,2″-terthienyl, and 2-chloro-4-[5-(penta-1,3-diynyl)-2-thienyl]but-3-ynyl acetate in the presence of near ultraviolet (u.v.) radiation (320–380 nm). Conidiogenesis in A. niger, and sporangiosporogenesis in R. nigricans were depressed on media treated with 2,2′: 5′,2″-terthienyl and irradiated with near u.v. light. Radial growth of mycelia of all fungi tested was dramatically reduced by all three compounds in the presence of near u.v. light. The viability of conidia of A. niger, and R. nigricans was unaffected by 2,2′: 5′,2″-terthienyl, both in the dark and in near u.v. light. Newly emergent germ-tubes were most sensitive to toxicity mediated by u.v. light. The oomycetous fungi tested were the most sensitive to the photo-activated toxicity generated by the three compounds used. The results indicate that ED50 values are dependent upon the species and the presence or absence of near u.v. light. Dramatically lowered ED50 values were always observed in all systems treated with near u.v. light. The dose of near u.v. light used had no effect on the radial growth of fungi in the absence of the three compounds.  相似文献   

7.
Benomyl [methyl 1-(butylcarbamoyl)-benzimidazol-2-ylcarbamate] (350 × 10?6 M) decreased the respiration rate of Fusarium oxysporum conidia by 50% during germination. This inhibition was maintained at least 24 h after the treatment had begun. The treatment did not modify the relation between incubation time and respiration rate. Carbendazim [methyl benzimidazol-2-ylcarbamate], thiabendazole[2-(thiazol-4-yl)benzimidazole], thiophanate [1,2-di-(3-ethoxycarbonyl-2-thioureido)benzene] and thiophanate-methyl [1,2-di-(3-methoxycarbonyl-2-thioureido)benzene] were assayed using isolated mitochondria of Saccharomyces cerevisiae. These four compounds decreased mitochondrial respiration and oxidative phosphorylation rates to different extents when they were applied at a concentration of 250 × 10?6 M . Thiophanate-methyl was the most effective since it completely suppressed the mitochondrial respiratory control at 75 × 10?6 M .  相似文献   

8.
Ammonium sulphate and urea, but not potassium sulphate, increased the persistence of carbaryl in a flooded laterite soil with a low native nitrogen content (0.04%), but not in an alluvial soil with a higher nitrogen content (0.11%). Thus, NH4+ but not SO42-, contributed to the increased persistence of carbaryl. Likewise, ammonium sulphate increased the persistence of carbofuran in the laterite soil, but not in the alluvial soil. Significant accumulations of 1-naphthol and 2,3-dihydro-2, 2-dimethylbenzofuran-7-ol (‘carbofuran phenol’), in soils treated with carbaryl or carbofuran, suggested hydrolysis as the major pathway of degradation. Treatment of the two soils with ammonium sulphate, urea or potassium sulphate led to a decrease in soil-bound residues and an increase in the respective hydrolysis products, compared with untreated soils. Sorption studies indicated that NH4+ and SO42- compete with carbaryl, 1-naphthol and carbofuran for sorption and exchange sites in the complex soil system. Evolution of [14C]carbon dioxide from ring-14C in carbaryl and carbofuran was negligible. Consequently, after 40 days, more than 50% of the 14C in [14C]carbaryl and [14C]carbofuran remained in the soils as hydrolysis products (1-naphthol or 2,3-dihydro-2,2-dimethylbenzofuran-7-ol) plus soil-bound residues.  相似文献   

9.
Differential accumulation of [14C]imazalil and [14C]fenarimol by germlings of wild-type and DMI-resistant isolates ofPenicillium italicum was studied at various pH values. At pH 7 and 8 the low-resistant isolate E300–3 accumulated 22% and 35%, respectively, less imazalil than the wild-type isolate W5. Imazalil accumulation at pH 5 and 6 was similar. Isolate E300–3 also accumulated less fenarimol as compared with the wild-type isolate. This difference was much more obvious than for imazalil and was observed at all pH values tested. Differences in accumulation of both imazalil and fenarimol between low (E300–3), medium (H17) and high resistant (I33) isolates were not observed. These results suggest that decreased accumulation of DMIs is responsible for a low level of resistance only and that additional mechanisms of resistance might operate in isolates with a medium and high degree of resistance. With all isolates fenarimol accumulation was energy-dependent. This was not obvious for imazalil.The wild-type and DMI-resistant isolates had a similar plasma membrane potential as determined with the probe [14C]tetraphenylphosphonium bromide ([14C]TPP+). Various test compounds, among which ATPase inhibitors, ionophoric antibiotics and calmodulin antagonists, affected the accumulation of [14C]TPP+, [14C]imazalil and [14C]fenarimol. No obvious correlation between the effects of the test compounds on accumulation levels of the fungicides and [14C]TPP+ could be observed. These results indicate that the plasma membrane potential does not mediate the efflux of DMI fungicides byP. italicum.  相似文献   

10.
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   

11.
Radioactive dinitramine (1) was incorporated at 12 Ib/acre (0.6 ppm) in Anaheim silty loam soil and its degradation studied over an 8-month period. For both specifically—14CF3 and -Ring-UL-[14C] labeled (1), only ca. 20% of the radioactivity was lost from the incorporated zone. Mehanol- or acetonitrile-extractable radioactivity decreased rapidly over the initial 60 days reaching 20% after 244 days. Two compounds were isolated and characterized as (1), 0.05 ppm, and 6-amino-1-ethyl-2-methyl-7-nitro-5-trifluoromethylbenzimidazole (2), 0.06 ppm. Two other compounds were tentatively identified by TLC as monodealkylated dinitramine (3), 0.01 ppm, and 6-amino-2-methyl-7-nitro-5-trifluoromethylbenzimidazole (4), 0.01 ppm, Sodium hydroxide (10%) and anionic surfactant (10%) were effective in removing up to 50% of the residual bound radioactivity (i.e., nonacetonitrile extractable), while dimethylamine (25%) released 26%; extraction by acid was less effective.  相似文献   

12.
Following intraperitoneal administration to male mice of trichlorphone, 4 mg/animal = 160 mg/kg and butonate, 5 and 10 mg/animal = 200 and 400 mg/kg, labeled by 14C in the OCH3-groups, nucleic acids taken from different organs and urine were analyzed for [7-14C]methylguanine. The limit of detection was 2 × 10?8, calculated as 14C relative to the total dose. The maximum of 14C in 7-methylguanine was 2 × 10?7 in lung, kidney, and testicles and 3 × 10?6 in liver. The excretion rate of 7-MeG from nucleic acids is very rapid, a halflife of 2.0 hr was measured in liver from butonate and of < 24 hr was calculated in the whole body from trichlorphone, contrary to the excretion rate of 3.0–3.5 days following administration of strongly genotoxic agents. The relative amounts of [7-14C]methylguanine excreted in the urine were determined and compared with data for dichlorvos, dimethyl sulfate, and methyl methanesulfonate from the literature. Following intraperiotoneal administration, the methylating capability towards N-7 of guanine in nucleic acids is given by the ratio of about 100:10:25 for dichlorvos, butonate, and trichlorphone, respectively.  相似文献   

13.
植物土传病原菌拮抗细菌的筛选与鉴定   总被引：11，自引：2，他引：11  
从作物根际土壤中分离到1056株细菌，筛选出7个具有较强拮抗活性的菌株。室内测定对水稻纹枯病菌、辣椒疫病菌、瓜果腐霉、油菜菌核病菌、棉花枯萎病菌、茄根腐病菌、棉花黄萎病菌、番茄青枯病菌、甘蓝黑腐病菌等重要土传病原菌有较强拮抗作用；温室盆栽试验对番茄青枯病表现出较好防效，其中以BOH2和OH11效果较为明显，防效分别为90．9％和86．4％。通过形态观察、生理生化试验和16SrDNA序列分析，确定OH11为产酶溶杆菌。BOH3为荧光假单胞菌，其余5个菌株为不同芽孢杆菌。  相似文献   

14.
[目的]从当归内生真菌中筛选抗小麦赤霉病菌、番茄早疫病菌、番茄灰霉病菌、水稻纹枯病菌等植物病原菌的有益菌株,并筛选代谢产物中的抑菌活性部位.[方法]采用平板拮抗法对抗性菌株进行初步筛选,采用抑制菌丝生长法以及抑制孢子萌发法筛选有益内生真菌代谢产物中的抑菌活性部位.[结果]抗小麦赤霉病菌、番茄早疫病菌的内生真菌较多,分别占24.3％和28.6％.对小麦赤霉病菌、番茄早疫病菌、番茄灰霉病菌以及水稻纹枯病菌生长抑制作用较强的内生真菌包括5个属8个菌株,其中6个菌株只对1种病原菌菌丝生长有抑制作用.此外,对4种植物病原真菌孢子萌发具有抑制作用的内生真菌超过20％,其中内生真菌Myxormia sp.2和Myxormia sp.4的提取物对4种植物病原真菌孢子萌发的抑制作用显著,抑制率达到90％以上.通过对有益内生真菌代谢产物的分析表明,乙酸乙酯提取部位对植物病原真菌菌丝体和孢子萌发的抑制作用相对较强.[结论]具有抗菌活性的当归内生真菌及其次生代谢产物具有丰富的多样性.  相似文献   

15.
Several series of alkyl-substituted amino-, bromo-, chloro-, fluoro- and hydroxy-1, 4-naphthoquinones, as well as some 6-alkylaminoquinoline-5, 8-diones and 7-alkyl-6-hydroxyquinoline-5, 8-diones were prepared and tested as protectant fungicides against apple powdery mildew (caused by Podosphaera leucotricha). While most of the compounds did not reduce infection when applied at 10?3M, several 3-alkyl-2-bromo-and 3-alkyl-2-chloro-1, naphthoquinones were found to have ED50 values below 50 × 10?5M.  相似文献   

16.
The reactivation of the rat brain muscarinic acetylcholine receptor (mACh-R) binding with dimercaptosuccinic acid (DMSA) after in vitro and in vivo inhibition by mercuric chloride (HgCl2) and methylmercuric chloride (MeHg) was investigated. Receptor binding was estimated by the potent and specific antagonist l-[3H]quinuclidinyl benzilate ([3H]QNB). Rat brain synaptosomal membranes were exposed to HgCl2 and MeHg. At 1 × 10?4M. HgCl2 caused complete inhibition of the [3H]QNB binding. The inhibition of [3H]QNB binding by HgCl2 was still higher than 50% at 1 × 10?8M. MeHg caused less inhibition of [3H]QNB binding than HgCl2. The inhibited receptors showed a significant degree of reactivation when treated with DMSA. The recovery was almost complete after MeHg inhibition or with the lower HgCl2 concentrations. Generally, the reactivation was dependent on the concentration of DMSA. When rats injected with either early or delayed doses of DMSA following administration with five consecutive daily doses (8 mg/kg body wt, Gavage method) of MeHg or HgCl2, the inhibition of [3H]QNB binding was less than untreated ones. The early treatment with DMSA decreased the inhibition of [3H]QNB binding due to MeHg or HgCl2 intoxication. However, DMSA was more effective in reducing HgCl2 inhibition than MeHg either in vitro or in vivo treatment. The ability of DMSA to reactivate the mACh-R after inhibition with the mercurials emphasizes the involvement of essential sulfhydryl groups in [3H]QNB binding sites, and also shows that these sulfhydryl groups are the primary target for the MeHg and HgCl2 inhibition of the rat brain muscarinic receptors.  相似文献   

17.
The metabolism of [14C]asulam (methyl 4-aminophenylsulphonylcarbamate), [14C] aminotriazole (1H-1,2,4-triazol-3-ylamine) and [14C]glyphosate (N-(phosphonomethyl)glycine) were assessed in Equisetum arvense L. (field horsetail). Following application of the test herbicides (4mg?0.3 °Ci herbicide/shoot) to the shoots of 2-year-old pot-grown plants, the total recovery of 14C-label after 1 week and 8 weeks was high for all three herbicides (>80-0% of applied radioactivity). Asulam was persistent (>69-7% of recovered radioactivity) in both shoots and rhizomes. Sulphanilamide, a hydrolysis product of asulam, accounted for the remainder of the recovered radioactivity. Aminotriazole showed evidence of conjugation in shoots and rhizomes. The principal 14C-labelled component in shoots was composed of high proportions of aminotriazole (>76-3%) together with the metabolites: X (ninhydrin positive), β-(3-amino-1,2,4-triazolyl-1-)α-alanine, Y (diazotization positive) and various unidentified compounds. Rhizomes generally contained lower proportions of intact aminotriazole (>59.4%) together with the metabolites X,Y and unidentified compounds. The proportion of aminotriazole did not decrease with time in shoots or rhizomes; however, the ratio of metabolite X: Y moved in favour of Y as the interval after treatment increased. Glyphosate was extensively metabolised in shoots and rhizomes to yield aminomethylphosphonic acid (AMPA) and various unidentified compounds. Differential metabolism appears to be one of the factors which may govern the persistence and toxicity of the test herbicides in E. arvense.  相似文献   

18.
The interactions of natural pyrethrins and nine pyrethroids with the nicotinic acetylcholine (ACh) receptor/channel complex of Torpedo electric organ membranes were studied. None caused significant reduction in [3H]ACh binding to the receptor sites, but all inhibited [3H]perhydrohistrionicotoxin ([3H]H12-HTX) binding to the channel sites in presence of carbamylcholine. Allethrin inhibited [3H]H12-HTX binding noncompetitively, but [3H]imipramine binding competitively, suggesting that allethrin binds to the receptor's channel sites that bind imipramine. The pyrethroids were divided into two types according to their actions: type I, which included pyrethrins, allethrin, bioallethrin, resmethrin, and tetramethrin, was more potent in inhibiting [3H]H12-HTX binding and acted more rapidly (i.e., in <30 sec). Type II, which included permethrin, fluvalinate, cypermethrin and fenvalerate, was less potent and their potency increased slowly with time. Also, inhibition of the initial rate of [3H]H12-HTX binding by type I compounds increased greatly by the presence of the agonist carbamylcholine, but this was not so with type II compounds. The receptor-regulated 45Ca2+ flux into Torpedo microsacs was inhibited by pyrethrins and pyrethroids, suggesting that their action on this receptor function is inhibitory. There was very poor correlation between the potencies of pyrethrins and pyrethroids in inhibiting [3H]H12-HTX binding and their toxicities to house flies, mosquitoes, and the American cockroach. However, the high affinities that several pyrethroids have for this nicotinic ACh receptor suggest that pyrethroids may have a synaptic site of action in addition to their well known effects on the axonal channels.  相似文献   

19.
Choiromyces aboriginum Mü1w1c6是一株分离自芦苇的拮抗内生真菌。通过离体平板对峙培养检测和光学、电子显微镜观察,以及测定在活体植物上的拮抗活性,研究芦苇内生真菌Choiromyces aboriginum Mü1w1c6与病原菌及其寄主植物黄瓜之间的相互作用。对峙培养显示出较强的营养和空间竞争能力,对病原菌菌丝生长抑制率多高于60％,对立枯丝核菌Rhizoctonia solani的抑制率达到100%。显微观察证明它与多种病原菌有缠绕等重寄生现象。在互作研究中,C.aboriginum Mü1w1c6可成功定殖于黄瓜苗的根部,预先接种能有效抑制瓜果腐霉Pythium aphanidermatum在黄瓜根部组织细胞内的扩展和定殖,对P.aphanidermatum引起的黄瓜苗期猝倒病有良好的防效,接种一次内生菌防治效果为44.29%,接种两次生防效果高达88.49%。结果表明,C.aboriginum Mü1w1c6对多种植物病原真菌具有广谱的拮抗活性,对黄瓜苗期猝倒病具有较好的生防潜力。  相似文献   

20.
A base-promoted cyclisation of 4-nitroso-5-benzylsulphonamidopyrazoles (VII) afforded 6 H -pyrazolo[3,4-c][1,2,5]thiadiazine-2,2-dioxides (VIII). They were tested in vitro for antifungal activity against a series of phytopathogenic fungi of different taxonomic classes. Five of the compounds had noteworthy activity; in particular 6H-3-phenyl-5-methyl-7–(3,4-dichlorophenyl) pyrazolo[3,4-c][1,2,5]thiadiazine-2,2-dioxide (VIIIc) at the concentration of 200 mg litre?1 completely inhibited the growth of Pythium ultimum, Corticium solani and Sclerotinia minor.  相似文献   

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