Resistance problems and environmental stresses promote the discovery of agrochemicals with novel structure and mechanism. Bioisosterism is widely employed in the rational modification of lead agrichemical compounds, being used to increase potency, enhance selectivity, improve physicochemical properties, eliminate resistance and toxicity, and acquire novel chemical space to secure intellectual property. The insecticide chlorantraniliprole, which has two amides as the characteristic structure, is one of the top-selling insecticides globally. It can effectively control lepidopteran pests by targeting ryanodine receptors (RyRs). Examples of modification by replacing aliphatic amide with bioisostere in Chlorantraniliprole has been continuous reported. The α-subsitituted alcohol bioisostere has been shown to mimic the electronic and electrostatic properties, of an amide bond. In this research, α-subsitituted alcohols were introduced to replace aliphatic amide of chlorantraniliprole. Derivatives of the alcohol were also investigated. The design, synthesis, biological activity, SAR analysis, molecular docking of chlorantraniliprole analogues containing α-substituted alcohol and its derivatives will be presented.

Design, synthesis and insecticidal activities of Chlorantraniliprole analogues containing α-subsitituted alcohol and its derivatives

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ACS Fall 2022

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