Abstract

New options for pest insect control, including new insecticides, are needed to ensure a plentiful food supply for an expanding global population. Any new insecticides must meet the increasingly stringent regulatory requirements for mammalian and environmental safety, and also address the need for new chemistries and modes of action to deal with resistance to available insecticides. As underscored by a paraphrase of a quote from Louis Pasteur “Chance favors the prepared mind”, the agrochemical industry uses a variety of approaches that attempt to improve on “chance” for the discovery of new insecticides. Although there are a number of approaches to the discovery of new insecticidal active ingredients (AIs), historically most insecticides are based on a pre-existing molecule or product either from a competitor or from an internal company source. As such the first examples of a new insecticide representing a new type or class of AI (First-in-Class: FIC) are important as prototypes for other AIs stimulating further spectrum, efficacy, physicochemical, and environmental safety refinements. FIC insecticides also represent a measure of innovation. Understanding the origins of these FIC compounds and the approaches used in their discovery can provide insights into successful strategies for future new classes of insecticides. This perspective will focus on an analysis of the approaches that have been used for discovery of FIC insecticides highlighting those approaches that have been the most successful and providing a reference point for current and future directions.

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