AbstractThe importance of biomass as a source of chemicals, biofuels, and energy is widely accepted. Currently, the attention is mainly focused on the valorisation of by-products from lignocellulosic materials. Chemical compounds derived from plants and microorganisms that provide good protection for crops against weeds, pests, and diseases (biopesticide active substances) have been used to formulate pesticides. Their use is increasingly encouraged by new pesticide regulations that discourage the use of harmful active substances. This article reviews the current and future situation of biopesticides, especially natural chemical products, and focuses on their potential within the European pesticide legislative framework. Moreover, this article highlights the importance of the different modes/mechanisms of action of the active substances obtained from natural sources, the role of chemistry in biopesticide development, and how the adoption of integrated pest management practices contributes to a greater trend towards biopesticides.