In keeping with our investigation, a simple and practical synthesis of novel heterocyclic compounds with a sulfamoyl moiety that can be employed as insecticidal agents was reported. The compound 2-hydrazinyl-N-(4-sulfamoylphenyl)-2-thioxoacetamide 1 was coupled smoothly with triethylorthoformate or a variety of halo compounds, namely phenacyl chloride, chloroacetyl chloride, chloroacetaldehyde, chloroacetone, 1,3-dichloropropane, 1,2-dichloroethane, ethyl chloroformate, 2,3-dichloro-1,4-naphthoquinone, and chloroanil respectively, which afforded the 1,3,4-thiadiazole and 1,3,4-thiadiazine derivatives. The new products structure was determined using elemental and spectral analysis. Under laboratory conditions, the biological and toxicological effects of the synthetic compounds were also evaluated as insecticides against Spodoptera littoralis (Boisd.). Compounds 3 and 5 had LC50 values of 6.42 and 6.90 mg/L, respectively. The investigated compounds (from 2 to 11) had been undergoing molecular docking investigation for prediction of the optimal arrangement and strength of binding between the ligand (herein, the investigated compounds (from 2 to 11)) and a receptor (herein, the 2CH5) molecule. The binding affinity within docking score (S, kcal/mol) ranged between -8.23 (for compound 5), -8.12 (for compound 3) and -8.03 (for compound 9) to -6.01 (for compound 8). These compounds were shown to have a variety of binding interactions within the 2CH5 active site, as evidenced by protein-ligand docking configurations. This study gives evidence that those compounds have 2CH5-inhibitory capabilities and hence may be used for 2CH5-targeting development. Furthermore, the three top-ranked compounds (5, 3, and 9) and the standard buprofezin were subjected to density functional theory (DFT) analysis. The highest occupied molecular orbital-lowest unoccupied molecular orbital (HOMO-LUMO) energy difference (ΔE) of compounds 5, 3, and 9 was found to be comparable to that of buprofezin. These findings highlighted the potential and relevance of charge transfer at the molecular level.

Quantifying compatibility among control agents is essential for development of integrated pest management (IPM). Chrysoperla carnea (Siemens) and insect growth regulator insecticides are widely used in IPM of Lepidoptera. C. carnea is a generalist predator naturally present in the Mediterranean agroecosystems and bred in insectariums for commercial purposes. Here, we evaluated lethal and sublethal effects of tebufenozide on C. carnea under laboratory conditions. The treatment of eggs with tebufenozide 24 or 48 h after they were laid did not affect the hatching rate or survival of the neonate larvae. Toxic effects of tebufenozide on topically treated larvae was low; development times of surviving larvae and pupae decreased significantly compared with controls. In choice bioassays, a high percentage of third-instar larvae chose prey (Spodoptera littoralis) treated with tebufenozide in preference to untreated prey. Moreover, second-instar larvae of C. carnea that had previously consumed tebufenozide-treated prey (0.75 mL/L) had significantly reduced larval development time compared with controls, while longevity of surviving adults, fecundity and egg viability were unaffected. Ingestion of tebufenozide by adults of C. carnea at the recommended field dose had no significant effect on female fecundity, egg viability or adult longevity. Tebufenozide exhibited low toxicity towards the developmental stages of C. carnea and is therefore a candidate for inclusion in IPM strategies.

Staphylococcus aureus is a leading cause of prosthetic joint infections (PJI) characterized by bacterial biofilm formation and recalcitrance to immune-mediated clearance and antibiotics. The molecular events behind PJI infection are yet to be unraveled. In this sense, identification of polymorphisms in bacterial genomes may help to establish associations between sequence variants and the ability of S. aureus to cause PJI. Here, we report an experimental nucleotide-level survey specifically aimed at the intergenic regions (IGRs) of the icaADBCR locus, which is responsible for the synthesis of the biofilm exopolysaccharide PIA/PNAG, in a collection of strains sampled from PJI and wounds. IGRs of the icaADBCR locus were highly conserved and no PJI-specific SNPs were found. Moreover, polymorphisms in these IGRs did not significantly affect transcription of the icaADBC operon under in vitro laboratory conditions. In contrast, an SNP within the icaR coding region, resulting in a V176E change in the transcriptional repressor IcaR, led to a significant increase in icaADBC operon transcription and PIA/PNAG production and a reduction in S. aureus virulence in a Galleria mellonella infection model. In conclusion, SNPs in icaADBCR IGRs of S. aureus isolates from PJI are not associated with icaADBC expression, PIA/PNAG production and adaptation to PJI.

BACKGROUND: Chrysoperla carnea (Neuroptera: Chrysopidae) is a voracious predator frequently used in biological control programs to suppress pest populations of economic importance. However, it performs its duty in a challenging environment where various stress factors such as non-target effects of insecticides limit expected outcomes. A study providing details of genetics, cross-resistance, realized heritability, and stability of insect growth regulators (IGRs) resistance such as pyriproxyfen in this bio-control agent is essential.
RESULTS: Selection with pyriproxyfen, an IGR, resulted in 3092.10-fold and 39.60-fold resistance when judged against Susceptible and Field Pop, respectively. Very low cross-resistance to buprofezin while no cross-resistance to acetamiprid and spinosad was observed. Incompletely dominant, autosomal and polygenic resistance was also associated with high realized heritability (h2 = 0.35). Furthermore, resistance to pyriproxyfen was stable in this bio-control agent.
CONCLUSIONS: These findings make Chrysoperla carnea an ideal fit in integrated pest management (IPM) programs where biological control approaches are employed in combination with IGRs sprays to control various insect pests especially Whitefly, Bemisia tabaci. Releasing pyriproxyfen-resistant Chrysoperla carnea in a multi-sprayed cropping environment would help to keep pest population below economic threshold level. It would also minimize risk of insecticide resistance development in pests surviving even after several insecticide applications. © 2020 Society of Chemical Industry.

Synergistic effects of octopamine receptor agonists (OR agonists) have attracted many scientists based on their potent effects on mosquitoes. Herein, we determined the toxicity of selected insect growth regulators (IGRs) on fourth instar larvae of Culex quinquefasciatus. We evaluated the synergistic action of OR agonists on the toxicity of IGR insecticides to achieve a better understanding of their mode of action. As a result, pyriproxyfen was the most potent IGR insecticide (EC50 = 0.049 ng/ml) followed by lufenuron, novaluron, and diflubenzuron according to the IGR bioassay. Further, based on the acute bioassay, lufenuron was the most toxic IGR insecticide (LC50 = 44 ng/ml) after 24-h post treatment followed by pyriproxyfen, novaluron, and diflubenzuron (LC50 = 137, 263, and 1127 ng/ml, respectively). Similar tendency was observed after 48 and 72-h post treatment. Furthermore, OR agonists that combined with pyriproxyfen was the most significant effects after 48 and 72-h of exposure. The synergism with amitraz (AMZ) was more significant when co-treated with IGR insecticides compared to chlordimeform (CDM). These findings suggest that OR agonists are promising tools and are important alternative strategies as synergistic compounds in preventing and controlling Culex quinquefasciatus mosquitoes.

In the standard ISO soil toxicity test using Collembola, adult survival and juvenile production are the only endpoints that can be attainable. The information on egg production and egg hatching cannot be investigated in the ISO test. To overcome this limitation, in this study, the effects of teflubenzuron on life history parameters of Yuukianura szeptyckii (Collembola) were investigated with a compressed soil test. Teflubenzuron is an insect growth regulator and has a negative effect on egg production, and egg hatching process of arthropods. LC50 decreased with increases in exposure period from 6.97 mg/kg in the third week to 3.60 mg/kg in the fourth week. The EC50 for egg and juvenile production was 0.57 mg/kg and 0.26 mg/kg, respectively. The hatching rate decreased significantly from 46 to 7% as the concentration increased from 0.25 to 1.00 mg/kg, respectively, and the molting frequency was significantly affected only at > 4 mg/kg. The toxic contribution rate (TCR) was defined as the ratio of juvenile production at an exposure concentration compared with the control, and a simple life history model was developed for TCR estimations. At the lower concentrations (< 0.3 mg/kg), the hatching rate reduction was a main contributor to the total toxicity, but the adult mortality and egg production reduction were the main contributors at the higher concentrations (> 2.0 mg/kg). The contribution of egg production reduction remained relatively constant. Since collembolan populations in the soil can be composed of various developmental stages, the differences in the sensitivity to chemicals depending on the developmental stages should be included in the assessment of the toxic impact on soil ecosystems.

Immature stages of the boll weevil, Anthonomus grandis grandis Boh. (Coleoptera: Curculionidae), develop protected inside cotton fruiting structures. Therefore, the adult beetles have become the main target of insecticide applications. The use of insect growth regulators (IGRs) is recommended against immatures, even though they may also affect the survival and reproductive traits of adult insects. The present study evaluated the impact of a juvenile hormone analog (pyriproxyfen), an ecdysteroid agonist (methoxyfenozide), and a chitin biosynthesis inhibitor (lufenuron) on adult cotton boll weevils, a key cotton pest. Mated and virgin beetles were treated by feeding them contaminated squares and cotton leaf discs that were previously immersed into pyriproxyfen, methoxyfenozide, and lufenuron solutions at field-rate concentrations. After exposure, treated couples were caged onto cotton plants, and survival, fecundity, and egg viability were evaluated. The IGRs neither affected the survival nor fecundity of adult boll weevils. On the other hand, egg viability was significantly reduced by lufenuron, regardless of whether the females were treated premating or postmating or whether their pairs were either treated or untreated. However, egg viability increased as the females aged since the initial exposure date to lufenuron, indicating a potential transovarial effect of this insecticide. Our results indicate that pyriproxyfen and methoxyfenozide do not affect adult boll weevils, whereas lufenuron temporarily reduces the egg viability of this key cotton pest.

Allatostatins (AST) are neuropeptides originally described as inhibitors of juvenile hormone (JH) synthesis in insects. Consequently, they have been considered as potential lead compounds for the discovery of new insect growth regulators (IGRs). In the present work, receptor-based three-dimensional quantitative structure-activity relationship (3D-QSAR) was studied with 48 AST analogs, and a general approach for novel potent bioactive AST analogs is proposed. Hence, six novel AST analogs were designed and synthesized. Bioassays indicated that the majority novel analogs exhibited potent JH inhibitory activity, especially analog A6 (IC50: 3.79 nmol/L), which can be used as lead compound to develop new IGRs.

The synergistic action of octopamine receptor agonists (OR agonists) on many insecticide classes (e.g., organophosphorus, pyrethroids, and neonicotinoids) on Aedes aegypti L. has been reported recently. An investigation of OR agonist\'s effect on insect growth regulators (IGRs) was undertaken to provide a better understanding of the mechanism of action. Based on the IGR bioassay, pyriproxyfen was the most potent IGR insecticide tested (EC50=0.0019ng/ml). However, the lethal toxicity results indicate that diafenthiuron was the most potent insecticide (LC50=56ng/cm(2)) on A. aegypti adults after 24h of exposure. The same trend was true after 48 and 72h of exposure. Further, the synergistic effects of OR agonists plus amitraz (AMZ) or chlordimeform (CDM) was significant on adults. Among the tested synergists, AMZ increased the potency of the selected IGRs on adults the greatest. As results, OR agonists were largely synergistic with the selected IGRs. OR agonists enhanced the lethal toxicity of IGRs, which is a valuable new tool in the field of A. aegypti control. However, further field experiments need to be done to understand the unique potential role of OR agonists and their synergistic action on IGRs.

Studying insecticide resistance in mosquitoes has attracted the attention of many scientists to elucidate the pathways of resistance development and to design novel strategies in order to prevent or minimize the spread and evolution of resistance. Here, we tested the synergistic action of piperonyl butoxide (PBO) and two octopamine receptor (OR) agonists, amitraz (AMZ) and chlordimeform (CDM) on selected novel insecticides to increase their lethal action on the fourth instar larvae of Aedes aegypti L. However, chlorfenapyr was the most toxic insecticide (LC50 = 193, 102, and 48 ng/ml, after 24, 48, and 72 h exposure, respectively) tested. Further, PBO synergized all insecticides and the most toxic combinatorial insecticide was nitenpyram even after 48 and 72 h exposure. In addition, OR agonists significantly synergized most of the selected insecticides especially after 48 and 72 h exposure. The results imply that the synergistic effects of amitraz are a promising approach in increasing the potency of certain insecticides in controlling the dengue vector Ae. aegypti mosquito.