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Article Abstract

2-Methylquinazolin-4(3)-one was prepared by the reaction of anthranilic acid, acetic anhydride, and ammonium acetate. The reaction of 2-methylquinazolin-4(3)-one with -aryl-2-chloroacetamides in acetone in the presence of potassium carbonate gave nine -aryl-2-(2-methyl-4-oxoquinazolin-3(4)-yl)acetamide compounds. The structures of these compounds were elucidated on the basis of their IR, H nuclear magnetic resonance (NMR), C NMR, and high-resolution mass spectrometry (HR-MS) spectral data. These synthesized compounds containing the 2-methyl-3,4-dihydroquinazolin-4-one moiety exhibited activity against mosquito larvae with LC values of 2.085-4.201 μg/mL after 72 h exposure, which is also confirmed using a quantitative structure-activity relationship (QSAR) model. Interestingly, these compounds did not exhibit toxicity to the nontarget organism . In silico molecular docking revealed acetylcholine binding protein (AChBP) and acetylcholinesterase (AChE) to be potential molecular targets. These data indicated the larvicidal potential and environmental friendliness of these -aryl-2-(2-methyl-4-oxoquinazolin-3(4)-yl)acetamide derivatives.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10357533PMC
http://dx.doi.org/10.1021/acsomega.3c01686DOI Listing

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