Nonsteroidal ecdysone agonists.

Abstract

Nonsteroidal ecdysone agonists are novel compounds that have become attractive candidates not only as pest control agents in agriculture but also as tools for research. Their narrow spectrum of activity makes them relatively safe as pesticides, and their mode of action as ligands for gene expression has found application in gene therapy and inducing transgenic gene expression in plants. These diacylhydrazines (DAHs) are potent nonsteroidal ecdysone agonists, and four of them, tebufenozide, methoxyfenozide, chromafenozide, and halofenozide, have been developed as insecticides. Although these compounds are very toxic to insects, they are safe for mammals and are environmentally benign. Their action on insects is also selective, the first three are effective against Lepidoptera but weakly active or inactive on Diptera and Coleoptera. On the other hand, halofenozide is effective on Coleoptera but mildly active on Lepidoptera. Previous reviews on ecdysone agonists have concentrated on the biological response of some DAHs and their effects on pests. In this review, the chemistry, biological effects and their modes of action at the molecular level will be covered. In addition, a few studies on other nonsteroidal ecdysone agonists, such as 3,5-di-tert-butyl-4-hydroxy-N-iso-butylbenzamide, acylaminoketones, and benzoyl-1,2,3,4-tetrahydroquinolines, will be briefly reviewed.