Du Tan, Yiping Wang, Wulin Yang, Xusheng Shao, Zhong Li
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Design, Synthesis, and Insecticidal Evaluation of Neonicotinoid Analogues With 1,2-Dihydropyridine Scaffold
A series of neonicotinoid analogues with 1,2-dihydropyridine scaffold were synthesized by the novel annulation reaction. Bioassay indicated that some compounds exhibited good insecticidal activity against Aphis craccivora at a concentration of 100 mg/L, and the substituents on the phenyl group have a great influence on insecticidal activity. Especially, the LC50 values of compounds A3 and A19 were 17.089 and 4.792 mg/L, respectively. Molecular docking results revealed that compound A19 bound to Lymnaea stagnalis acetylcholine binding protein via H-bonds with the residues of Leu102, Val114, and Arg55. These results proposed a promising guide for the design of neonicotinoid analogues with 1,2-dihydropyridine scaffold.
期刊介绍:
The Journal of Heterocyclic Chemistry is interested in publishing research on all aspects of heterocyclic chemistry, especially development and application of efficient synthetic methodologies and strategies for the synthesis of various heterocyclic compounds. In addition, Journal of Heterocyclic Chemistry promotes research in other areas that contribute to heterocyclic synthesis/application, such as synthesis design, reaction techniques, flow chemistry and continuous processing, multiphase catalysis, green chemistry, catalyst immobilization and recycling.