Structure-activity relationship and mode of action study of insect growth regulators

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A number of N,N′-dibenzoyl-N-t-butylhydrazine analogs containing various substituted benzoyl moieties were synthesized and their biological activity was measured using various biological systems. Larvicidal activity against Chilo suppressalis, Spodoptera exigua, and Leptinotarsa decemlineata was measured. In addition, the molting hormone activity was estimated by the ability to stimulate N-acetylglucosamine incorporation into cultured integument fragments from C. suppressalis larvae. Binding affinity to the receptor was assayed using proteins prepared by in vitro translation of the responsible cDNA cloned from a cell-free preparation of larval tissue of C. suppressalis or L. decemlineata. Binding to intact Sf-9 cells, which can be regarded as an index of the receptor binding, was also measured. Variations in the biological activity indices were either analyzed using physicochemical, molecular and substituent parameters or correlated between two different activity types. Comparisons among correlations clearly indicate the physicochemical and biological meaning of parameters significant in the correlation equations to increase our understanding of the molecular mechanism of molting hormones.

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