Quantitative structure-activity studies of benzoylphenylurea larvicides: II. Effect of benzyloxy substituents at aniline moiety against Chilo suppressalis Walker

The larvicidal activity of a series of N-2,6-difluorobenzoyl-N′-[4-(substituted benzyloxy)-phenyl]-ureas against nondiapause larvae of the rice stem borer, Chilo suppressalis Walker, was measured by a topical application method under conditions in which oxidative metabolism was inhibited by piperonyl butoxide. The effects of the substituted-benzyloxy moiety on variations in the activity were analyzed quantitatively using physicochemical substituent parameters and regression analysis. Results were compared with those found previously for N-2,6-difluorobenzoyl-N′-(4-substituted phenyl)-ureas, indicating that the electron-withdrawing property of the anilide substituents participates in determining the activity through the inductive effect. The hydrophobicity of the total anilide substituents favors activity, whereas the steric dimension in terms of the width lowers it. Although inhibition of new cuticle formation on cultured integument of diapausing larva could not be determined accurately for most of the compounds because of their limited solubility in the assay medium, inhibitory activity seemed related to larvicidal activity, as was the case for previously investigated simpler congeners.     

Quantitative structure-activity studies of substituted benzyl chrysanthemates: 5. Physicochemical substituent factors and neurophysiological effects in knockdown and lethal activities against the house fly

Knockdown and lethal activities of meta- and para-substituted benzyl (1R)-trans-chrysanthemates against the house fly were measured under synergistic conditions using piperonyl butoxide as an inhibitor of oxidative metabolism and NIA 16388 as an inhibitor of hydrolytic degradation. The variations in these activities were quantitatively analyzed in terms of physicochemical substituent effects using electronic, hydrophobic, and steric parameters of the aromatic substituents, and regression analysis. The most significant parameter in determining these activities is the steric bulkiness represented by the van der Waals voluem, the effect of which is highly specific to substituent positions. The substituent effects on knockdown and lethal activities against the house fly are shown to correspond well, respectively, with those on the convulsive and lethal activities against the American cockroach. The relationship between these symptomatic activities against the house fly and the neurophysiological activities determined by using excised nerve cords from American cockroaches were also quantitatively analyzed. Each house fly symptomatic activity was found to be analyzable by a linear combination of the neuroexcitatory and neuroblocking activity indices when the transport factor was separated by using the hydrophobicity parameter.     

Spread of local electroantennogram response of the European corn borer, Ostrinia nubilalis

The electroantennogram (EAG) responses of male moths of the European corn borer (Ostrinia nubilalis) to locally applied pheromone, (Z)-11-tetradecenyl acetate, were studied with multiple electrodes. The amplitude of the locally elicited EAG was different depending on the stimulated point and also on the recorded locus, and a gradient in the amplitude was observed along the antennal axis. The locally stimulated region responded as a local negative deflection relative to the resting region, and the response spread from the stimulated point in an asymmetric way, more effectively in the proximal direction than in the distal direction. A possible mechanism of the local EAG spread is discussed.     

Effect of oral administration of 3,3',4,4',5-pentachlorobiphyenl on the intestinal microbiota of Sprague–Dawley rats

The effect of the endocrine-disrupting chemical 3,3',4,4',5-pentachlorobiphyenl (PCB 126) on intestinal microbiota after oral administration, and the improvement of intestinal microbiota and feces quantity by the subsequent administration of Lactobacillus acidophilus or Lactobacillus reuteri was investigated. All the rats were given 100 μg/kg bodyweight of PCB 126. The changes in bacterial counts were confirmed using a culture method. The administration of PCB 126 tended to decrease the bacterial counts of lactobacilli (10^9.6−10^10.2 to 10^8.8−10^9.2) and bifidobacteria (10^5.3−10^6.1 to 10^3.6−10^4.2), and to increase those of Enterobacteriaceae (10^8.2−10^9.1 to 10^9.4−10^10.3) and staphylococci (10^6.6−10^7.4 to 10^7.2−10^8.4) compared to no PCB 126 administration. After administration of PCB 126, L. acidophilus or L. reuteri orally administered to rats caused Enterobacteriaceae and staphylococci counts to decrease, suggesting that the intestinal microbiota was improved by the lactobacilli. The administration of L. acidophilus and L. reuteri improved the balance of intestinal microbiota, and defecation volume returned to its normal level. L. acidophilus and L. reuteri have a remedial effect on intestinal microbiota affected by PCB 126 and can function to lessen accumulated PCB 126 volume.     

Quantitative structure—activity relationships of light-dependent herbicidal 4-pyridone-3-carboxanilides I. Effect of benzene ring substituents at the anilide moiety

A number of substituted 4-pyridone-3-carboxanilide derivatives show various degrees of light-dependent herbicidal activity. The effects of substituents at the anilide moiety on the activity against Echinochloa oryzicola were analysed quantitatively with physicochemical substituent parameters. The activity was shown to vary parabolically with total hydrophobicity (Σπ) of the anilide ring substituents as well as with the steric parameter (E_s) of the ortho-substituents. The E_s parameter for only the bulkier ortho-substituent, with the more negative value, but not for the two, was significant. The effect of substituents at the 1-position was expressible by indicator variables assigned to each 1-substituted series, the physicochemical rationalization being left for future analyses.     

Quantitative structure-activity relationships of light-dependent herbicidal 4-pyridone-3-carboxanilides III. 3-D (comparative molecular field) analysis including light-dependent diphenyl ether herbicides

Using a set of representative members selected from 4-pyridone-3-carboxanilides and ortho-chlorinated diphenyl ethers exhibiting light-dependent herbicidal activity, we examined the three-dimensional structure-activity relationships quantitatively. The most stable conformation of each compound, regarded as the ‘active conformation’, was determined by either semi-empirical or ab initio molecular orbital calculations. With a hypothesis defining a common substructural skeleton between the two different compound series. each molecule was superimposed. We first analysed the structure-activity relationship using an index for the substructure shape similarity according to the superimposed conformations. After finding the relevance of the hypothesis, we examined the three-dimensional structure-activity relationship using the comparative molecular field analysis procedure. The results suggested that the two different series of compounds have a common region of the receptor site. The variations in the light-dependent herbicidal potency were governed by hydrophobicty and three-dimensional steric and electronic field parameters of molecules participating in the transport process and the interaction with the receptor site. The result was consistent with that derived from our previous quantitative analysis with the use of free-energy-related substituent parameters and the traditional regression procedure for a large number of pyridone-carboxanilides.     

Mechanism of neuromuscular block by chlordimeform

The mechanism of action of chlordimeform on the frog sciatic nerve-sartorius muscle preparation has been studied by means of microelectrodes. Chlordimeform (0.1 mM) suppresses the amplitude of spontaneous miniature end-plate potentials without much changing their frequency. At 1 mM, it completely blocks the miniature end-plate potentials. The resting membrane potential is not affected. The end-plate potential evoked by nerve stimulation is also suppressed, while the action potential from the nerve terminal is not impaired. The sensitivity of the end-plate membrane to the transmitter substance as examined by iontophoretic applications of acetylcholine is effectively decreased by chlordimeform. The quantal content of transmitter release is not affected. It is concluded that the block of neuromuscular transmission by chlordimeform is due primarily to a depression of the end-plate sensitivity to the transmitter.     

Quantitative structure-activity study of herbicidal N-aryl-3,4,5,6-tetrahydrophthalimides and related cyclic imides

The quantitative relationship between structure and inhibitory activity against the root growth of sawa millet of 30 N-aryl-3,4,5,6-tetrahydrophthalimides and 88 related N-aryl cyclic imide compounds (3-aryl-1,5-tetramethylenehydantoins, 4-aryl-1,2-tetramethylenetriazolidine-3,5-diones, and their thiocarbonyl analogs) was analyzed by means of physicochemical parameters of the aryl substituents and regression analysis. The results showed that, in each series of these classes of compounds, the position-specific steric effects of aromatic substituents, as represented by Verloop's STERIMOL values, are highly important in determining the inhibitory potency of the compound.     

Development of furnished cages re‐using conventional cages for laying hens: Behaviour,physical condition and productivity

Furnished cages for laying hens have advantages in allowing normal behaviors and maintaining productivity. As the cost of introduction is a barrier for farms, we developed furnished cages that re‐use conventional cages. To determine the minimum and functional cage design, we compared six designs, combinations of two floor designs (artificial turf or wire cage floor) and three screening designs in the integrated area (no screening, one entrance side or four sides). In total, 144 hens were used, and we measured behavior, physical condition and productivity. Comparing the floors, the percentages of hens performing dust‐bathing and laying eggs in the integrated area were higher in cages with turf than wire floor (P < 0.05 for both). Comparing the screening, dust‐bathing, litter‐exploring and active behavior tended to be more frequent in cages with the integrated area screened on one side than four sides. Feather damage was lower in cages with the integrated area screened on one side than with no screening (P < 0.05). These results suggest that the cage design with an integrated area with artificial turf floor, screened on one side, was effective for furnished cages that re‐use conventional cages.