bluuebunny/crossref_metadata_2025_split huggingface dataset:
Structure—activity relationships in pyrethroid esters derived from substituted 2‐phenoxy‐3‐methylbutanoic acids
Authors: Nisha George , Kalyanasundaram Muthuswamy 
Published: November 2006

AbstractNon‐cyclopropane pyrethroid esters of different substituted 2‐phenoxy‐3‐methylbutanoic acids have been synthesised using the three alcohols—3‐phenoxybenzyl alcohol, α‐cyano‐3‐phenoxybenzyl alcohol and 3, 4‐methylene‐dioxybenzyl alcohol. Among the 35 esters synthesised and tested against Culex quinquefasciatus Say, the Bancroftian filariasis vector, for both larvicidal and adulticidal activities, α‐cyano‐3‐phenoxybenzyl 2‐(4‐fluorophenoxy)‐3‐methylbu‐tanoate, with an LC50 value of 2.5 × 10−3 mg litre−1 for larvicidal activity, and α‐cyano‐3‐phenoxybenzyl‐2‐(4‐chlorophenoxy)‐3‐methylbutanoate, with an LD50 value of 30 times; 10−4 ug insect−1 for adulticidal activity, were found to be as effective as fenvalerate, a well‐known non‐cyclopropane pyrethroid ester. Structure‐activity studies showed that the insecticidal activity is dependent on the nature and position of the substituent in the phenyl ring of the acid moiety and also on the type of alcohol moiety.
Multivariate structure‐property relationships (MSPR) of pesticides
Authors: Domine Daniel , Devillers James , Chastrette Maurice , Karcher Walter 
Published: November 2006

AbstractVapour pressures, aqueous solubilities, n‐octanol/water partition coefficients, molecular weights, and Henry's law constants for 64 pesticides were obtained from the literature and analysed by means of Principal Component Analysis (PCA). Classical PCA displays underline structure‐property relationships. However, interpretation of PCA requires reference to the original data matrix and comparisons made between every point. To overcome this problem, a novel graphical approach, based on collections of maps encoding the chemical and structural information included in the original data set, was used to interpret the results. Multivariate analyses coupled to graphical tools were useful for interpreting physicochemical properties of pesticides in terms of multivariate structure‐property relationships (MSPR).
Inhibition of Echinochloa crus‐galli var. frumentacea seedling root elongation by chiral 1, 3, 5‐triazines in the dark
Authors: Omokawa Hiroyoshi , Konnai Makoto 
Published: November 2006

Abstract2‐z‐Substituted benzylamino‐4‐substituted‐amino‐6‐chloro‐1,3, 5‐triazines are herbicidal compounds showing leaf‐burning and/or growth inhibition with concomitant greening and stunting. Effects of chiral 1,3,5‐triazine compounds in a light‐independent seedling root elongation test with Echinochloa crus‐galli var. frumentacea Wight demonstrated an interaction between chirality and root growth inhibition. The test compounds inhibited root growth, and this inhibition was due to interference with a system or systems other than photosynthesis. 4‐(R)‐sec‐butylamino‐2‐(α,α‐dimethylbenzyl)amino‐6‐chloro‐1,3, 5‐triazine showed the highest inhibitory activity, and 4‐methylamino‐2‐(R)‐a‐methylbenzylamino‐6‐chloro‐1,3,5‐triazine was second. The chiral requirement for a strong inhibition of root growth was the (R)‐configuration, contrasting with the requirement for the (S)‐configuration for an inhibition of photosystem II.
Rhizome‐induction activity of chiral 2‐α‐methylbenzylamino‐4‐alkylamino‐6‐chloro‐1, 3, 5‐triazines in Cyperus serotinus Rottb.
Authors: Omokawa Hiroyoshi , Takeuchi Masaaki , Konnai Makoto 
Published: November 2006

AbstractA cytokinin‐like effect of chiral 2‐α‐methylbenzylamino‐4‐alkylamino‐6‐chloro‐1,3,5‐triazines was found using a rhizome‐inducing assay with Cyperus serotinus Rottb. tubers. C. serotinus tubers germinated in distilled water yielded plantlets with roots and leaves. Secondary rhizomes were normally not observed within the regular 14‐day incubation time in water culture, whereas after increasing incubation periods a very short rhizome appeared (controls). 6‐Benzylaminopurine (BA) significantly stimulated rhizome induction, while other plant hormones were inactive. The (R)‐isomers of the 1, 3, 5‐triazine compounds also stimulated induction of the rhizomes, whereas the (S)‐isomers did not. The described rhizome induction system seems to be suitable as a cytokinin bioassay. The (R)‐1, 3, 5‐triazine compounds showing rhizome‐inducing activity (RI activity) inhibited root formation and plant growth at high concentrations with symptoms which were very similar to those of BA. Therefore, the (R)‐isomers appear to act as cytokinins in the rhizome induction assay.
Degradation of the dicarboximide fungicides iprodione, vinclozolin and procymidone in Patumahoe clay loam soil, New Zealand
Authors: Slade E. Ann , Fullerton Robert A. , Stewart Alison , Young Harry 
Published: November 2006

AbstractAn enhanced rate of degradation of the dicarboximide fungicides iprodione and vinclozolin was induced in the laboratory in Patumahoe clay loam soil by adding three successive applications of fungicide. Enhanced degradation of the dicarboximide fungicide procymidone could not be induced. Following the first fungicide treatment, the time to 50% loss of iprodione was greater than 35 days; for vinclozolin the time to 50% loss was 22 days. The rate of degradation accelerated with successive applications until, after a third successive application of fungicide, the time to 50% loss of iprodione was only two days and none was detectable at seven days. For vinclozolin, after the third successive application of fungicide, 50% loss occurred after 35 days. By comparison, minimal loss of procymidone was detected after 35 days following each of two successive soil treatments.The induction of enhanced degradation of iprodione and vinclozolin in this soil in the laboratory may explain the observed loss of field control of onion white rot disease. Degradation of iprodione occurred in non‐sterile soil but not in sterile soil, indicating that microbial involvement may be responsible for the degradation of iprodione and vinclozolin in soil.
Insecticide resistance in cotton aphid Aphis gossypii (Glov.) in the Sudan Gezira
Authors: Gubran El Mahi E. , Delorme Robert , Augé Dnielle , Moreau Jean P. 
Published: November 2006

AbstractThe resistance to insecticides of three Sudanese strains of A. gossypii (Glov.) collected from cotton fields in the Sudan Gezira Scheme over three seasons (1988, 1989, 1990) and that of two French strains was studied in the laboratory. When compared with a known susceptible strain, the aphids were found to be resistant‐to the eight insecticides tested. Evolution of resistance in Sudanese strains during the three crop seasons was observed. Assay of aphid homogcnate for carboxytesterase activity towards the substrates α‐naphthyl acetate and β‐naphthyl acetate showed that there was no enhancement of this class of enzyme and thus it was not a cause of resistance in this species. A study of interaction between the acetylcholinesterase (AchE) and pirimicarb established the kinetics of the inhibition process. I50 values were found to be much higher for the Sudanese strains than for the susceptible strain. First‐order inhibition kinetics revealed that resistance towards pirimicarb in Sudanese‐strains was caused by a modified AchE which had a reduced affinity (higher Ka value) and poor carbamylation ability (lower K2 value) for pirimicarb. The resistance mechanisms for the other insecticides remain to be studied.
Influence of temperature, soil moisture and soil characteristics on the persistence of alachlor
Authors: Walker Aiian , Moon Young‐Hee , Welch Sarah J. 
Published: November 2006

AbstractAlachlor degradation in soils followed first‐order reaction kinetics. Half‐lives in moist soil varied from 11.30 to 34.8 days at 25°C to 95.9 to 279.6 days at 5°C, and at 15°C varied from 15.7 to 83.1 days at 5 kPa soil water stress (field capacity) to 82.8 to 281.4 days at 1500 kPa (permanent wilting point). Degradation rates in laboratory incubations with fluctuating temperatures were predicted with reasonable accuracy from the constant‐temperature data. The degradation rate and extent of adsorption were lower in subsoils than in soils from the plough layer. Degradation rate was positively correlated with microbial biomass and microbial respiration, and adsorption was positively correlated with soil organic matter content. Persistence of alachtor in field plots was correlated well with variations in weather pattern during the period September 1990 to July 1991, with an effective half‐life varying from 20 to 60 days. Persistence in the field plots was predicted accurately by a computer model of herbicide behaviour.
Fate of the benzoylphenyl urea CGA‐184699 in the cat flea Ctenocephalides felis
Authors: Zakson Michelle , Hink W. Fred , MacKichan Janis J. 
Published: November 2006

AbstractHPLC was used to determine levels of the benzoylphenyl urea, CGA‐184699, in cat blood, flea faeces and eggs. Rate constants were determined for the decline of CGA‐184699 concentration in flea faeces of fleas that fed on both high (696 ng ml−1) and low (305 ng ml−1) host blood concentrations. There were strong correlations between the concentration of the drug in the host's blood and in flea eggs, between egg concentration and egg hatch and between the concentration of CGA‐184699 in faeces and mortality to larvae feeding upon faeces.
Phagodeterrent response of the bulb mite Rhizoglyphus robini to various pyrethroids and some of their cleavage products
Authors: Cohen Ephraim , Joseph Tamar 
Published: November 2006

AbstractFeeding‐avoidance response of the bulb mite Rhizoglyphus robini to various insecticidal and acaricidal pyrethroids and some of their cleavage products was examined using a two‐choice cellulose disc bioassay. The mites were able to detect extremely low quantities of certain pyrethroids, down to 1–5ng of pesticide applied to a cellulose disc weighing 200 mg. The phagodeterrent potency of the pyrethroids was found to be in the following decreasing order: fenvalerate > cypermethrin > deltamethrin > bioresmetnrin > pyrethrin > bifenthrin > cis‐permethrin > trans‐permethrin. Fenpropathrin, bioallethrin, flucythrinate and tetramethrin were stimulatory up to a level of 50 ng disc−1. A 100‐ng dose of fenpropathrin deterred the mites. Chemical and photochemical cleavage products of pyrethroids possessed phagodeterrent potencies comparable to those of the intact pesticides. 3‐Phenoxybenzotc acid and cis‐chrysanthemic acid were the most effective deterrents followed by dibromochrysanthemic acid and the cis and trans bifenthrin acid moiety. The probable relevance of the observed phagodeterrence by pyrethroid residues and their cleavage products, as related to induction of dispersal and eventual outbreaks of mites, is discussed.
Synthesis and bioactivity of some fluorine‐containing benzoyl arylureas. Part I: Insecticidal‐acaricidal products in which the aryl group bears a trifluoromethyl‐substituted alkyl or alkenyl side chain
Authors: Meazza Giovanni , Rama Franco , Bettarini Franco , Piccardi Paolo , Massardo Pietro , Caprioli Vincenzo 
Published: November 2006

AbstractThis paper reports the synthesis and the biological activity of benzoyl arylureas in which the aryl group bears a trifluoromethyl‐substitiited alkyl or alkenyl side chain, R. The activity of these compounds has been evaluated on larvae of S. littoralis, A. aegypti, L. decemlineata and on the eggs of T. urticae. In general: (1) the optimum insecticidal activities are achieved when the substituents on the benzoyl moiety, R1, and R2, are 2,6‐difluoro, the substituents on the aryl moiety, R3, are 3,5‐dichloro and R1, is 4‐(CHC(CI)CF3); (2) the best acaricidal activity is shown when R1, is 2‐CI, R2, and R3, are hydrogen atoms and R1, is 4‐(CH2CH2CH(CI)CF3); (3) the best overall activity is displayed when R1, is 2‐CI, R2 is hydrogen, R3 is 3‐chloro and R1 is 4‐(CH2CH2CF3).
Effects of oxadixyl treatment on the ultrastructure of Phytophthora infestans infecting tomato leaves
Authors: Jiang Yong 
Published: November 2006

AbstractOxadixyl is a systemic fungicide controlling diseases caused by Oomycetes. In this ultrastructural study of the mode of action, it was found that more than 40% of 60 observed haustoria of Phytophthora infestans were less than I am in diameter in tomato leaf inner spongy mesophyll tissues previously treated with the fungicide (8 μg ml‐1) and were on average smaller than in untreated tissues. Ultrastructural observations on treated tissues also revealed that dictyosome vesicles were fewer near dictyosomes in the region of the intercellular hyphae which subtended the haustorium and in haustoria, during haustorium development. Fungal nucleoli degenerated and. in contrast to previous observations of the fungitoxic effects, numbers of ribosomes decreased in the cytoplasm, indicating that synthesis of ribosomes was probably inhibited. In addition, fragmentation of the endoplasmic reticulum and increases in the number and size of vacuoles and lomasomes were also observed in treated tissues. These results were considered to be fungistatic effects of the fungicide on the fungus. In some infected plant cells, electron‐dense deposits appeared in the cytosol in the vicinity of the extrahaustorial membrane. Compared with the nature of the related compound, metalaxyl, there appear to be differences between their effects in some aspects, e.g. haustorium development and haustorial encasement formation.
Evaluation of volatile allyl alcohol derivatives for control of snails on cut roses for export
Authors: Ittah Yitzhak , Zisman Uzi 
Published: November 2006

AbstractAllyl alcohol esters (propionate, formate, and acetate) and structurally related compounds (3‐methylallyl alcohol and vinyl acetate) were evaluated for their fumigation properties vis‐a‐vis Theba pisana (Mueller) snails.The esters were very effective in exterminating the snails, although less so than the parent alcohol. These results suggest that the esters might first have to undergo hydrolysis, and only thereafter demonstrate their potency. 3‐Methylallyl alcohol (four‐carbon member) and vinyl acetate (two‐carbon member, after hydrolysis) were significantly less potent than the allyl esters. All three esters showed less phytotoxicity towards roses than did allyl alcohol itself. However, only allyl acetate caused no damage whatsoever to the entire plant tested (flower, leaves, sepals, and stem).
Disposition kinetics, cytotoxicity and residues of fenvalerate in tissues following oral administration to goats
Authors: Mandal Tapan K. , Bhattacharya Anjan , Chakraborty Animesh K. , Basak Dipak K. 
Published: November 2006

AbstractDisposition kinetics in goats of fenvalerate [(RS)‐α‐cyano‐3‐phenoxybenzyl (RS)‐2‐(4‐chlorophenyl)‐3‐methylbutyrate] were studied after oral administration at 5 mg kg−1. The insecticide persisted in blood for up to 48 h. The Vd(area), t1/2(β), and t1/2(Ka), of fenvalerate were 12.14 (±0.39) litre kg−1, 12.25 (±0.25) h and 0.63 (±0.11)h, while the AUC and ClB values were respectively 7.35 (±0.39) μg h ml−1 and 0.68 (±0.04) litre kg−1 h−1. The residues in tissues reached a peak four days after insecticide administration and then started to decline. Maximum residue was found in the adrenal gland, followed by liver, kidney and intestine. Both GOT and GPT activities in kidney tissue, but only GPT activities in liver tissue had decreased significantly 4, 8 and 22 days post‐administration. The fenvalerate did not produce any significant effects on serum acetylcholinesterase, cholesterol or protein levels in goats. Histopathological examination showed fatty changes in the periphery of lobule, congestion in sinusoid, haemolysis in central vein, necrosis and periportal fibrosis around the central vein of liver, and necrosis in kidney of fenvalerate‐treated goats.
Selection, inheritance and characterization of carbofuran resistance in the Colorado potato beetle (Coleoptera: Chrysomelidae)
Authors: Ioannidis Philippos M. , Grafius Edward J. , Wierenga Joel M. , Whalon Mark E. , Hollingworth Robert M. 
Published: November 2006

AbstractThe objectives were to select for resistance to carbofuran in a susceptible field population of Colorado potato beetles, Leptinotarsa decemlineata (Say), assess the progression of resistance, and characterize the inheritance and possible mechanism of resistance. Initial selection in the field resulted in over 99.9% mortality of treated larvae but high resistance in the survivors. Subsequent laboratory selection at c.80% mortality increased resistance to > 100‐fold by the fourth generation. Low level cross‐resistance to azinphos‐methyl was also present. Resistance appeared to be inherited via a single, autosomal, incompletely dominant gene, resulting in decreased acetylcholinesterase sensitivity. A second Michigan population also appeared to exhibit reduced cholinesterase sensitivity. Resistance to carbofuran in a Colorado potato beetle population from Long Island, NY appears to involve primarily mixed‐function oxidase enzymes. The history of insecticide use probably affects which primary resistance mechanism appears in response to carbofuran treatment.
Negative cross‐resistance to N‐phenylanilines in benzimidazole‐ resistant strains of Botrytis cinerea, Venturia nashicola and Venturia inaequalis
Authors: Josepovits Gyula , Gasztonyi Maya , Mikite Gyula 
Published: November 2006

AbstractA new series of compounds with high contra‐selective activity against benomyl‐resistant fungal strains was found among ring‐substituted N‐phenyl‐anilines. Hydrophobic substitution in one of the benzene rings, together with the secondary amine character of the molecule, are important factors for high fungitoxicity. The sensitivities of benomyl‐resistant isolates to some representatives of the N‐phenylanilines equal or even surpass their sensitivity to diethofencarb or MDPC. The negative cross‐resistance with benzimdazole fungicides is valid for strains of Botrytis cinerea, Venturia nashicola and Venturia inaequalis. The strains of B. cinerea with double insensitivity to benzimidazoles and phenyl‐carbamates are insensitive also to N‐phenylanilines. However, the similarly double‐insensitive strain of V. nashicola was found to be just as sensitive to the N‐phenylanilines tested as the strain resistant only to benzimidazoles. The latter result revealed an important bonus compared with diethofencarb. Preventive application of one of the most active representatives of the N‐phenylanilines to young cucumber plants was effective against infection with benomyl‐resistant isolates of B. cinerea. Moderate apical translocation after root‐dipping was also observed.
Larval feeding and movement in two Plutella xylostella (Lepidoptera: Plutellidae) populations exposed to discrete deposits of permethrin
Authors: Adams Andrew J. , Hoy Casey W. , Hall Franklin R. , Nettleton Sara Y. 
Published: November 2006

AbstractFeeding and movement by two Ohio populations of diamondback moth (Plutella xylostella L.) on leaf discs treated with individually applied, uniformly‐sized droplets of permethrin was video‐recorded. Incorporation of fluorescent dye in the permethrin solution allowed comparison of the proportion of leaf area eaten with proportion of deposits consumed and measurement of distance travelled across the leaf surface between contacts with droplets. There was a direct relationship between proportion of leaf area eaten and proportion of deposits consumed (slope ∼ 1.0). Feeding by the more physiologically susceptible population was unaffected by drop size (100–220 μm, 50 drops disc−1 in each case) and the proportion of the leaf disc consumed was much less than that recorded for the more resistant population at the two smaller drop sizes (100 μm and 150 μm). These data indicate that the P. xylostella larvae showed no behavioural avoidance of deposits when feeding, but ingestion of permethrin inhibited feeding in the more susceptible population. Two equivalent measures of avoidance when moving, the average distance travelled between contacts with droplets and the average number of contacts per unit distance travelled, were not different for the two populations, indicating no difference in the average ability of insects from these populations to avoid deposits of permethrin. The average distance travelled and the average number of contacts with droplets during the 90‐min period was significantly greater for the more susceptible population, indicating that the behaviour of the two populations differed. These differences are consistent with a post‐contact irritation in the more physiologically susceptible larvae.
Kinetic and thermodynaimic aspects of the dye‐sensitised photo‐oxidation of bioresmethrin and related compounds
Authors: Clements Paul , Wells Clifford H. J. 
Published: November 2006

AbstractThe Rose Bengal sensitised photo‐oxidation of bioresmethrin (I), 2‐benzylfuran‐4‐ylmethyl acetate (II), and 2‐benzylfuran‐4‐ylmethanol (III) has been studied in methanol and methanol + water (1 + 1 by volume) solutions by monitoring the rate or oxygen removal from the system. The results indicate that the compounds studied are oxidised via reaction with singlet oxygen. Values for the rate constants for reaction of singlet oxygen with compounds I‐III have been determined over the temperature range 293–308 K, and the energy of activation and entropy of activation for the reactions have been determined. The data have been interpreted in terms of the site of attack of singlet oxygen on the compounds.
‘Pharmacokinetic’ and ‘pharmacodynamic’ design of lipophilic drugs based on a structural model for drug interactions with biological membranes
Authors: Herbette Leo G. 
Published: November 2006

AbstractThe pharmacokinetic profile a drug exhibits will ultimately depend on how the drug molecule interacts with the different cell membranes it encounters en route to its target site of action. Even if the drug molecule targets a soluble protein as its final site of action, there is a reasonable probability that it will interact with some cell membrane on its pathway to this biological target. In some cases, the final protein, lipid or sugar moiety target could be an integral part of the cell membrane architecture whereby the drug's interaction with the cell membrane could influence its pharmacodynamic profile as well, especially if the final site of action is an integral membrane‐bound receptor protein. In either case, drug transport across a cell membrane or within the cell membrane lipid bilayer compartment can dictate partial or dominant control of the drug's bioavailability. A molecular understanding of the equilibrium membrane partition coefficient, the rates of drug partitioning into and out of a cell membrane and the equilibrium location of the drug within the cell membrane can provide critical chemical design strategies for altering overall drug bioavailability and optimal pharmacokinetics.
Microcalorimetry and the Taylor—Aris method in the study of partition processes
Authors: Beezer Anthony E. , Mitchell John C. , Andrews David J. 
Published: November 2006

AbstractMicrocalorimetry is introduced briefly and shown to permit the development of biologically based Structure Activity Relationships (SARs). These data can be related to the more conventionally used parameter, the partition coefficient. Further, calorimetric studies are shown to allow comparison of the partitioning properties of biological cells with solvents that are normally used in drug partitioning studies. The results indicate that more consideration should be given to partitioning into particulate, e.g. micellar and liposomal, solvent systems. The use of the Taylor‐Aris dispersion broadening method is briefly introduced theoretically, and its practical exploitation is discussed.These two techniques, microcalorimetry and the Taylor‐Aris method are shown to allow new insights into partitioning systems and their application to biological SARs.