Background: The amino acids R- and S-proline were used to synthesize novel neonicotinoid derivatives that, after being characterized by H, DEPTQ 135, and HRMS-QTOF, were evaluated for use as insecticides against Galleria mellonella (caterpillar), Sitophilus zeamais, Xylosandrus morigerus, Xyleborus affinis, and Xyleborus ferrugineus.
Results: Comparisons of biological activity and absolute configuration showed that the R enantiomer had excellent and outstanding insecticidal activity against the insects tested, with up to 100% mortality after 12 h compared with dinotefuran at the same concentration.
Conclusions: The results suggest that compound R6 is an excellent lead enantiopure insecticide for future development in the field of crop protection. Furthermore, intermolecular interactions between nicotinic acetylcholine receptors and the R enantiomer displays a lower score which mean a higher affinity to the nAChR receptor and the π-π interactions are more stable than the S derivative. © 2023 Society of Chemical Industry.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1002/ps.7368 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Chlorfenapyr-related delayed rhabdomyolysis: a case series.
Front Neurol
January 2025
Department of Critical Care Medicine, The Fifth People's Hospital of Jinan City, Jinan, China.
Introduction: Chlorfenapyr, a broad-spectrum insecticide and acaricide of the pyrrole-class pesticides, can induce dizziness, fatigue, profuse sweating, and altered consciousness by interfering with cell energy metabolism. However, chlorfenapyr-related rhabdomyolysis has rarely been reported.
Case Presentations: Patient 1 was a healthy 26-year-old man who ingested approximately 30 mL of chlorfenapyr.
Evaluating the potential of Kalanchoe pinnata, Piper amalago amalago, and other botanicals as economical insecticidal synergists against Anopheles gambiae.
Malar J
January 2025
Caribbean Centre for Research in Biosciences, Natural Products Institute, University of the West Indies, Kingston, Jamaica.
Background: Synergists reduce insecticide metabolism in mosquitoes by competing with insecticides for the active sites of metabolic enzymes, such as cytochrome P450s (CYPs). This increases the availability of the insecticide at its specific target site. The combination of both insecticides and synergists increases the toxicity of the mixture.
View Article and Find Full Text PDFDiscovery of Novel Neonicotinoids with Conjugated Diene Enabled by Cascade Allylation/Isomerization Synthetic Methodology.
J Agric Food Chem
January 2025
Shanghai Key Laboratory of Chemical Biology & School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, P. R. China.
As one of the most significant insecticides, neonicotinoids have played a pivotal role in crop protection and public sanitation. However, the high resistance and bee toxicity of neonicotinoid insecticides have attracted considerable attention. Herein, a series of neonicotinoid compounds with conjugated diene moieties were synthesized through the cascade allylation/isomerization reaction.
View Article and Find Full Text PDFDesign and Process Considerations for Preparation of Modified Release Ivermectin and Praziquantel Tablets by Wet Granulation.
AAPS PharmSciTech
January 2025
University of Maryland, School of Pharmacy, Department of Pharmaceutical Sciences, 20 N Pine Street, Baltimore, Maryland, 21201, USA.
Dosage forms containing Ivermectin (IVER) and Praziquantel (PRAZ) are important combination drug products in animal health. Understanding the relationship between products with differing in vitro release characteristics and bioequivalence could facilitate generics. The goal of this study was to create granulations for each active ingredient, with similar release mechanisms, but substantially different in vitro release rates, and then compressing these granulations into tablets with differing release rates.
View Article and Find Full Text PDFTherapeutic Bioactivities and Chemical Composition Analysis of Rhizome Oleoresin of Hedychium coronarium Collected from Uttarakhand, India.
Comb Chem High Throughput Screen
January 2025
School of Pharmacy, D.Y. Patil University (Deemed to be University), Sector 7, Nerul, Navi Mumbai 400706, India.
Introduction: Hedychium coronarium J. König, from the Zingiberaceae family, is a rhizomatous herb used in Ayurvedic medicine for its febrifuge, anti-rheumatic, and anthelmintic properties.
Method: This study characterizes the chemical diversity and biological activities of H.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!