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1.
Ten 2-(substituted benzylidene)-7-(4-chlorophenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a]pyrimidin-3(7H)-one derivatives were synthesized and evaluated. A series of heterocyclic, 2-(substituted benzylidene)-7-(4-chlorophenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a]pyrimidin-3(7H)-one were synthesized by reaction of 7-(4-chloro phenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a]pyrimidin-3(7H)-one with appropriately substituted aldehydes in the presence of anhydrous sodium acetate and glacial acetic acid. The antinociceptive activity was evaluated by tail-flick technique, anti-inflammatory activity was evaluated by carrageenan-induced paw edema test and their ulcerogenicity index was determined. The para-substituted methyl, hydroxy, fluoro, chloro, bromo, and nitro derivatives showed significant antinociceptive and anti-inflammatory activities. The detailed synthesis, spectroscopic data, and pharmacological screening of the synthesized compounds were reported.  相似文献   

2.
Oxidation of aldehydes to carboxylic acids is a major reaction. Conventionally, this reaction is carried out with oxidants and metal catalysts, thus producing unwanted metal waste. Recently, aqueous media have been used as an alternative for toxic organic solvents. Here, we tested the clathrate-structured, neutral hydrogen peroxide adduct 4Na2SO4·2H2O2·NaCl for the oxidation of aldehydes to acids in aqueous solution. We found that various aromatic, heteroaromatic and aliphatic aldehydes were selectively oxidized to corresponding acids in 70–98% yields. This simple acid–base treatment allows to separate easily the acid product in high purity without any organic solvent. Moreover, the adduct is produced using 25% H2O2, with inexpensive sodium sulphate, Na2SO4, and sodium chloride, NaCl. The adduct is a non-toxic white crystalline solid, readily soluble in water, and easy to handle.  相似文献   

3.
The interactions of 10 different chromium(III) complexes with isolated calf thymus DNA have been analysed by studying the electronic and fluoresence spectra of intercalated ethidiumbromide. Triply charged cationic complexes including: [Cr(urea)6]Cl3.3H2O, [Cr(1,10‐phenanthroline)3](ClO4)3.2H2O, [Cr(2,2'‐bipyridyl)3] (ClO4)3.2H2O, [Cr(ethylendiamine)3]Cl3.3.5H2O and [Cr(NH3)6](NO3)3 displaced the dye from DNA. Similar effects were observed in experiments using the non‐intercalating dye bisbenzimidazole ("Hoechst 33258"). However, singly charged cationic, anionic and uncharged chromium(III) complexes such as: cis‐[Cr(1,10‐phenanthroline)2Cl2]Cl.2H2O, cis‐[Cr(2,2'‐bipyridyl)2Cl2]Cl.2H2O, [Cr(glutathione)2]Na2, [Cr(cysteine)2]Na.2H2O and [Cr(glycine)3] were unable to displace both ethidiumbromide and bisbenzimidazole from DNA. There was no evidence for the formation of co‐ordinate bonds between chromium(III) and DNA for any of the above complexes. The charge and type of ligand are important in controlling the interaction of chromium(III) with isolated DNA in vitro. Our findings indicate that the outer sphere interaction of a chromium(III) complex with DNA is weak and unlikely to be the mechanism by which chromate causes DNA impairments in vivo and in vitro.  相似文献   

4.
Summary. Doratomyces stemonitis (Hyphomycetales, Dematiaceae) is a saprotrophic fungus belonging to the mycobiota of the cereal rhizosphere. The fungus is able to metabolize benzoxazolin-2-(3H)-one and a variety of its derivatives including higher plant detoxification products, microbial degradation products and the chemically rather stable 2-amino-(3H)-phenoxazin-3-one. D. stemonitis can use all of these compounds as sole C-sources but their utilization, especially that of microbial degradation products and 2-amino-(3H)-phenoxazin-3-one, seems to be highly energy consuming, resulting in slow mycelium growth and a change of colony morphology. Benzoxazolin-2-(3H)-one derived compounds induce the synthesis of different isoforms of a glycosylated protein with sequence homologies to the endo-1,3-β-glucanase Asp f2, an allergen from Aspergillus fumigatus and other Asp f2-like proteins e.g., from Verticillium dahliae or PRA1 antigen from Candida albicans. The induction of the protein is regarded as a stress response.  相似文献   

5.
Three test-series were applied, which differed in regard to the basal medium (natural or artificial sea water, salinity level, addition of detergent); the culture conditions (primary cultures, subcultures, back-inoculations into basal medium without toxic metals); the criterion employed (zoospore activity, sporangia development, or dry weight of Thraustochytrium striatum Schneider). The temperature applied was 18° to 20°C. The sea water-pollen-method (MWP) proved to be the most suitable: it is simple and more sensitive than the other tests; subcultures and back-inoculations are possible without much additional work; conditions simulate nature; first results are available after 3 to 4 days. The SMS-method (enriched natural sea water of different salinities) provides additional information on salinity effects. Nine substances have been tested: (CH3COO)3Hg, HgCl2, CdCl2·H2O, ZnSO4 ·7H2O, NiSO4·7H2O, CuSO4·5H2O, CoCl2·6H2O, MnCl2 ·4H2O, and phenol. In regard to their toxicity these substances can be divided into 2 groups: Hg- and Cd-salts inhibit development down to greater dilutions than the remainder; Zn and Ni seem to yield intermediate effects. Salinity modifies the toxic effects of the test substances. In higher salinities, comparable concentrations of test substances reveal stronger inhibitory effects than in lower salinities. Detergents may augment the toxic effects, at least of CuSO4. The marine lower fungus T. striatum is a useful organism for testing biological consequences of water pollutants.  相似文献   

6.
2H-1,4-Benzoxazines are major heterocyclic compounds with interesting biological and synthetic applications. Therefore, it would be very interesting to develop new efficient methods for their synthesis. Here, we synthesized 2H-1,4-benzoxazines in one pot using K2CO3/H2O in the ionic liquid of choice, [omim][BF4]. After reactions, products are extracted from [omim][BF4] by Et2O and the ionic liquid is recovered and successfully reused over several recycles. Results show that high yields of 3-aryl-2H-1,4-benzoxazine derivatives are obtained chemoselectively at room temperature from their corresponding o-aminophenols and phenacyl bromides. To our knowledge, our method represents the most efficient and straightforward route for the synthesis of 3-aryl-2H-1,4-benzoxazine derivatives in short times and under environmentally benign conditions.  相似文献   

7.
Summary. During peak calling activity by male oil palm bunch moths, Tirathaba mundella Walker (Lepidoptera: Pyralidae), their hairpencils, wings or entire body were extracted in hexane. Gas chromatographic-electroantennographic detection (GC-EAD) analyses of hair pencil extracts revealed four compounds that consistently elicited responses from female antennae. The NMR spectrum of isolated compound 1, and mass spectra and retention indices of compounds 1–4 suggested that they were (3S,6S)-2,2,6-trimethyl-6-vinyl-tetrahydro-pyran-3-ol (1), 4-hydroxy-3-methoxy-benzaldehyde (2, vanillin), 6,10,14-trimethyl-2-pentadecanone (3), and 6,10,14-trimethyl-2-pentadecanol (4). Comparative GC and GC-MS analyses of hair pencils extract and synthetic standards confirmed these structural assignments. Moreover, comparative chromatography of synthetic and hairpencil-isolated 1 on a Cyclodex-B column (which separated the four stereoisomers with baseline resolution) revealed that male T. mundella produce the SS-stereoisomer (SS-1). In field cage bioassay experiments in Palembang, Indonesia, synthetic SS-1 and vanillin in combination, but not singly, attracted female T. mundella. SS-1 plus vanillin were as effective as male T. mundella in attracting females. Compounds 3 and 4 did not enhance the blend's attractiveness. Received October 11 2002; accepted March 14, 2003. R1D=" Correspondence to: Gerhard Gries, email: gries@sfu.ca  相似文献   

8.
The yellow-legged clearwing (YLC) Synanthedon vespiformis (Lepidoptera: Sesiidae) occurs in the Mediterranean and central Europe. It is polyphagous, boring into the woody parts of broadleaf species including forest trees as well as various Rosaceae species. S. vespiformis has been reported as an economically important pest causing severe injury to stone fruit plantations. Many attractants for sesiid species were discovered by random field screening using 2,13- and 3,13-octadecadienyl alcohols, acetates and aldehydes, including one for S. vespiformis; and about 20 sex pheromones of sesiids have been identified so far. In the present study we identified the natural composition of the sex pheromone of YLC laboratory reared females as a blend of E3,Z13- and Z3,Z13-octadecadienyl acetates, at a ratio of 4:1. We developed an efficient lure for monitoring the pest. Pheromone funnel traps with rubber septa, impregnated with 1 mg pheromone blend, efficiently captured males for 10 weeks. Suspension of Shin-Etsu? ropes containing a 2:1 blend of E3,Z13-18:Ac and Z3,Z13-18:Ac at 13.74 mg/ha/h, resulted in shutdown of trap catches in the treated plots and closely situated neighboring plots indicating that mating disruption is feasible.  相似文献   

9.
Micrometeorological measurements were made over an irrigated rice paddy during the Huaihe River Basin Experiment (HUBEX) in 1999. This study addresses the quality control and gap filling strategy for the heat fluxes with the Bowen ratio energy balance (BREB) method. It also endeavors to benefit future studies through comparing five methodologies to estimate the net water exchange. First, a three-step quality control strategy is constructed. Its first two steps guarantee the correct flux directions and reject suspicious data, respectively. The third step forbids supersaturation by considering the Bowen ratio ranges for different flux combinations (termed as “scenarios”). The quality-controlled latent heat (LE) and sensible heat (H) fluxes fall in three scenarios, namely I (LE > 0, H > 0), II (LE > 0, H < 0), and IV (LE < 0, H < 0). Second, the Priestley–Taylor evaporation model (PTEM) is applied to fill the gaps of LE, while the energy balance relationship is used to gap-fill H, namely H = R N GLE (R N : net radiation; G: soil heat flux). Central to the success of this strategy is the idea to calibrate the Priestley–Taylor parameter (α) in a scenario-specific manner. On average, α values are calibrated as 1.20 and 1.35 for scenario I and II, respectively. For scenario IV, most α values lie in a narrow range, namely from 0.9 to 1.0. Then, α is calibrated as 0.97 to extend the applicability of the PTEM to condensation (negative LE). The scenario-specific treatment explicitly explains the diurnal variation of α derived without distinguishing the scenarios. Third, five methodologies are compared in the calculation of net water exchange, including PTEM-gap-filled BREB method (M1), energy-balance-based eddy covariance method (M2), and three simplified models to estimate LE, respectively as R N H, R N G, and R N . A major finding is that G and H have a similar effect of about 3% in the net water exchange. Thus, if either is neglected, the net evaporation should be slightly lowered to avoid overestimate, by 3% as a rule of thumb from this work.  相似文献   

10.
Synthesis and characterization of Cu(II), Ni(II), and Zn(II) Schiff bases complexes resulted from the condensation of salicylaldehyde derivatives with o-amino phenol were discussed using elemental analysis (carbon, hydrogen, and nitrogen), molar conductance, magnetic measurements, mass spectra, and electronic spectra. The essential bands of infrared, 1HNMR, and UV-Vis spectra as well as thermogravimetric analysis corresponding to the active groups within the three ligands and their complexes were interpreted. The dehydration and decomposition processes of the [Cu(H2L1)(H2O)](OAc)2, [Ni(H2L1)(H2O)]SO4 · H2O, [Zn(H2L1)(H2O)]SO4 · H2O, [Cu(H2L2)(H2O)](OAc)2, [Ni(H2L2)(H2O)]SO4 · H2O, [Zn(H2L2)(H2O)]SO4 · 2H2O, [Cu(H2L3)(H2O)](OAc)2 · H2O, [Ni(H2L3)(H2O)]SO4 · 2H2O, [Zn(H2L3)(H2O)]SO4 complexes were studied thermodynamically using the integral method applying the Coats–Redfern and Horowitz–Metzger equations and the thermodynamic parameters were calculated. It was found from the elemental analysis and the thermal studies, that the ligand behaves as tridentate ligand forming chelates with 1 : 1 (metal : ligand) stoichiometrically. The molar conductance measurements of the complexes in dimethyl sulfoxide solvent indicate that the complexes have an electrolytic nature. The biological activities of the three ligands in comparison with metal(II) complexes were studied against different Gram positive and Gram negative bacteria.  相似文献   

11.
The stability, mixing and effect of downstream control on axisymmetric turbulent buoyant jets discharging vertically into shallow stagnant water is studied using 3D Reynolds-averaged Navier–Stokes equations (RANS) combined with a buoyancy-extended k –ε model. The steady axisymmetric turbulent flow, temperature (or tracer concentration) and turbulence fields are computed using the finite volume method on a high resolution grid. The numerical predictions demonstrate two generic flow patterns for different turbulent heated jet discharges and environmental parameters (i) a stable buoyant discharge with the mixed fluid leaving the vertical jet region in a surface warm water layer; and (ii) an unstable buoyant discharge with flow recirculation and re-entrainment of heated water. A stratified counterflow region always appears in the far-field for both stable and unstable buoyant discharges. Provided that the domain radius L exceeds about 6H, the near field interaction and hence discharge stability is governed chiefly by the jet momentum length scale to depth ratio lM/H, regardless of downstream control. The near field jet stability criterion is determined to be lM/H = 3.5. A radial internal hydraulic jump always exists beyond the surface impingement region, with a 3- to 6-fold increase in dilution across the jump compared with vertical buoyant jet mixing. The predicted stability category, velocity and temperature/concentration fields are well-supported by experiments of all previous investigators.  相似文献   

12.
Summary The host utilization process of insect parasitoids can be described by three stages of (1)habitatlocation, (2)host-location, and (3)host-acceptance andoviposition. There are 19 systems in which chemicals used inhabitat-location have been identified, 12 systems in which chemical cues leading tohost-location have been identified, and 16 systems in which chemicals elicitinghost-acceptance andoviposition have been identified. Both the chemical class and the source of the infochemical change with the stage of the host utilization process. Semiochemicals identified in thehabitatlocation stage were predominantly aldehydes, alcohols, sulfur-containing compounds, esters and terpenes, and were equally likely to be from the host-plant of the host, or from the host itself. Semiochemicals identified in thehost-location stage were sugars, alkanes, terpenes and heterocyclic aromatic compounds and 3/4 of them were host-produced cues. In thehost-acceptance andoviposition stage the identified semiochemicals were all produced by the host and were proteins, amino acids, triglycerides and salts. The importance of recognizing specific cues involved in host utilization by parasitoids is discussed, and suggestions for future research are made.  相似文献   

13.
A new biotechnological synthetic approach to 4-hydroxybenzoic acid is reported. Thauera aromatica cells produce the phenylphosphate carboxylase enzyme that selectively carboxylates phenylphosphate in the para position, without any formation of the ortho isomer. Here we show that the enzyme also works in supercritical carbon dioxide, opening a new technological solution to the recovery of the products that is a key problem when aqueous media are used. The enzyme shows an activity comparable with that shown under CO2 pressure in aqueous media and does not require the presence of NaHCO3.  相似文献   

14.
Clerodendrum indicum (L.) is one of the important medicinal plants, originating in India. The plant is used as medicine for bronchitis, asthma and different immunological disease. Micro-propagation is a quick method, producing a huge number of plants. Apical leaf of Clerodendrum indicum (L.) was used as an explant for callogenesis. The combinations of different plant growth regulators (2,4-D, NAA, KN) in MS (Murashige and Skoog) medium produced two types of calli: one was friable and loose and the other was green, embryogenic and compact. Heavy metals cause pollution and health hazards. The plant absorbs heavy metals, which is very useful for controlling environmental pollution. Iron is a major nutrient for both plants and animals, but hyper accumulation of iron is injurious to health. Calli were used to study the optimum conditions of iron uptake in presence of different chemical environments. The different environments were created by using different chemical reagents such as (HCL, HNO3, H3PO4 and KNO3). Iron (III) was spiked with radioactive Fe-59 and dynamics of uptake was followed by measuring radioactivity by gamma-ray spectrometer. The best condition of iron uptake corresponded to 1 mol L?1 KNO3 after 4 hour of equilibration.  相似文献   

15.
Observations of gonads and oocyte development stages (OS) have been achieved in Calanus helgolandicus females fed different algal diets and starved in filtered sea water under laboratory conditions during 8 days. The effects of 20 diets on egg production rates (EPR), hatching success (HS) and proportion of abnormal larvae (AL, development stages N1-2) were examined. With the control diet Prorocentrum minimum EPR and HS values were high, while AL was very low, coinciding with intact cell structures in oogonia (OO) and normal OS (OS1-OS4). With the other diets, oocyte maturation, EPR, HS and AL patterns were partially or totally impaired. Decrease of EPR coincided with the arrest of OS3 maturation and oocyte degradations, characterised by cell fragmentation, presence of apoptotic bodies in the OS3, degradation of cytoplasm in OS3 and OS4 and consequently the arrest of OS4 formation. These degradations were reversible when females were fed a favourable diet. Results reflect the presence of two distinct inhibitory mechanisms. Inhibition mechanism (1) impairs egg production. It was induced by starvation or by several species belonging to Bacillariophyceae (Chaetoceros calcitrans, Guinardia delicatula, Guinardia striata, Odontella regia, Rhizosolenia setigera, Stephanopyxis turris, Thalassiosira pseudonana) and mixed-diatom assemblages (collected in the field) and to the prymnesiophyte Pavlova lutherii. Remarkably other diatoms like Navicula sp., Nitzschia sp., Skeletonema costatum and Thalassiosira rotula did not induce mechanism (1) Inhibitory mechanism (2) affected exclusively HS and AL and was triggered by species independent of the production of polyunsaturated aldehydes (PUA), which are supposed to have adverse impacts on HS and larval development.  相似文献   

16.
Juveniles of Paragnathia formica Hesse (Isopoda; Gnathiidae) are haematophagous ectoparasites, feeding on fish blood which supplies the nutrients for their development through growth and moulting, and the subsequent survival and reproduction of the free-living adults. Little is known of the mechanisms of digestion in juvenile gnathiids, and biochemical studies on the digestive tract of these interesting estuarine isopods have not been undertaken previously. Here, functionally active cathepsin-like cysteine proteinases are identified in the digestive system of juvenile praniza (fed) and zuphea (unfed) forms. The physiological pH of the digestive tract and the optimum proteolytic activities detected in praniza 3 homogenates using the cathepsin B/L, cathepsin B, and cathepsin H fluorogenic substrates, N-Carbobenzoxy-Phe-Arg-4-methoxy-2-naphthylamine (Z-phe-arg-MNA), N-Carbobenzoxy-Arg-Arg-4-methoxy-2-naphthylamine (Z-arg-arg-MNA) and Arg-4-methoxy-2-naphthylamine (H-arg-MNA), respectively, are in the acidic range (pH 5.8–6.7). Inhibition profiles against Z-phe-arg-MNA and Z-arg-arg-MNA using the cathepsin B inactivator urea, and cysteine proteinase inhibitors, support the presence of cathepsin L- and B-like enzymes. These proteolytic activities are 10–50 times higher in homogenates of praniza 3 compared with zuphea 3 forms. Histochemistry of praniza 3 sections reveals that the predominant enzyme activity towards Z-phe-arg-MNA is limited to the digestive glands during early and mid stages of digestion; later, this activity appears in the lining of the anterior hindgut. Moreover, activity towards Z-arg-arg-MNA is generally restricted to the digestive glands, and only occasionally present in the anterior hindgut. In conclusion, the digestive glands are the main site of cathepsin-like cysteine proteinase activities in P. formica juveniles; these enzymes appear to be important to the digestion of host fish blood enabling development through to the free-living adult.  相似文献   

17.
Carbon dioxide and methane are major compounds involved in global warming. The process of CO2 and CH4 molecules absorption by water clusters was investigated by the molecular dynamics method. The frequency spectra of dielectric permittivity for systems consisting of (H2O) n , (CO2) i (H2O)10 and (CH4) i (H2O)10 clusters mixed in various proportions were determined. The IR radiation absorption spectra of these systems were calculated and compared. Also, the radiating power of these systems was established. The capture of greenhouse gases’ molecules by ultra disperse water media reduces the ability of the media to absorb the Earth’s radiation, i.e., it reduces the greenhouse effect.  相似文献   

18.
There are many industrial sites where open aggregate conical piles exist to store granular materials, like coal, industrial residuals, or other minerals. Usually these storage piles are placed in open areas, making them susceptible to wind erosion, which can create health, environmental, and/or economical concerns. It is common to minimize the dust emission through the placement of windbreaks in the vicinity of the storage piles, which reduces the wind speed in the vicinity of the pile’s surface. In this work, some experimental results from a wind tunnel study on the erosion of a conical sand pile, exposed or protected by a fence with porosities of 0, 70, and 83%, are shown. For the sheltered cases, the windbreak was placed at several distances from the pile’s leading edge, ranging from H to 4H, where H is the initial height of the non-eroded pile. The evolution of the shape of the sand pile is shown, at different instances in time, and the pile deformation quantified, using a novel experimental setup developed for wind erosion studies. This information might be regarded as a useful dataset for the benchmark of computational models aiming to produce the transient simulation of the aeolian erosion of stockpiles. The CFD results are comprised of the modeling of several experimental scenarios. The computational results for the surface wind velocity show a good correlation with the initial deformation of the pile. Based on the results, the isocontours of (u s /u r ) presented might be regarded as a good basis for the estimation of the pile shear velocity.  相似文献   

19.
Summary When the larvae of the caddis flyApatania fimbriata (Pictet) are threatened, drops of fluid appear on their head capsules. The secretions are produced in a gland in the dorsal part of the prothorax. The neck region contains an eversible sac with numerous single setae, groups of 3 setae, or rows of setae on the surface. The secretion is released through two paris of orifices on the lateral sides of the sac. For the most part the secretion is composed of some 30 fatty acids, with the major components having 12–14 carbon atoms and up to 4 double bonds (approx. 1–2 µg secretion per specimen). Biotests with synthetic saturated acids (C6–C12) in a stream and in the laboratory demonstrated a paralysing effect on small invertebrate predators (Rhyacophila sp.,Plectrocnemia conspersa, Hydropsyche sp., larvae, all Trichoptera). In choice experiments,Rhyacophila sp. larvae preferred larvae ofAgapetus fuscipes andDrusus annulatus (Trichoptera) as food as compared withApatania fimbriata larvae. Larger predators, such asDinocras cephalotes (Insecta, Plecoptera) and the fishCottus gobio, did not discriminate betweenApatania fimbriata and other prey species. The use of fatty acids in defensive secretions is interpreted as an adaptation to the running water environment. They are effective repellents againstRhyacophila sp. larvae, the most important predator in the natural environment ofApatania larvae.  相似文献   

20.
Photoelectro-Fenton was applied for the removal of acid yellow 36 (AY36) from synthetic aqueous solution using iron electrodes. A Box–Behnken design was used for optimization of the effects of pH, H2O2 concentration, current density, and reaction time. Individual effects of these variables were more important than their interaction effects. The derived model was in good agreement with the experimental results. Total organic carbon was determined in solution and sludge in order to clarify the removal mechanism. Increase of H2O2 concentration and current density led to domination of oxidation and coagulation mechanisms, respectively. The effects of scavenging and inhibiting agents were also investigated: (1) presence of alcohols can reduce the efficiency through competition with dye for reaction with hydroxyl radicals; (2) anions (NO3?, HCO3?, and H2PO4?) scavenged hydroxyl radicals and reduced decolorization of AY36.  相似文献   

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