2024
DOI: 10.1021/acs.jafc.4c00161
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Design of Inhibitors Targeting Chitin-Degrading Enzymes by Bioisostere Substitutions and Scaffold Hopping for Selective Control of Ostrinia furnacalis

Peibo Liang,
Jianyang Li,
Wei Chen
et al.

Abstract: Chitin-degrading enzymes are critical components in regulating the molting process of the Asian corn borer and serve as potential targets for controlling this destructive pest of maize. Here, we used a scaffold-hopping strategy to design a series of efficient naphthylimide insecticides. Among them, compound 8c exhibited potent inhibition of chitinase from Of Chi-h and Of ChtI at low nanomolar concentrations (IC 50 = 1.51 and 9.21 nM, respectively). Molecular docking simulations suggested that 8c binds to chiti… Show more

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