Status and outlook for acaricide and insecticide discovery

Abstract

To guarantee sustainability and progress, the agrochemical industry is faced with several major challenges. Currently, loss of active ingredients due to consumer perception, changing grower needs and ever-changing regulatory requirements is far higher than the number being introduced into the market. Therefore, there is a need to develop new products that can provide improved efficacy, selectivity and favorable environmental profiles. Strategies to achieve these goals are the search for acaricides and insecticides with new modes of action, or the discovery of novel molecules with activity on the most attractive target sites having resistance breaking properties against pest species. In this context, the introduction of halogen atoms or asymmetric centers into an active ingredient remains an important tool to modulate their properties, but so too is the pro-pesticide concept. This review gives an overview of agrochemicals launched over the past 8 years, reflects new insights into known mechanisms of action, and describes the status and outlook for acaricide and insecticide discovery. Supporting information may be found in the online version of this article.

Entomotoxic Activity of the Extracts from the Fungus, Alternaria tenuissima and Its Major Metabolite, Tenuazonic Acid

“…The absence of considerable behavior and developmental changes of the treated insects, lack of tremor, weak sensitivity of sucking phytophages, and clear antifeedant effect may indicate that TeA is not an inhibitor of lipid biosynthesis as spirotetramat is; instead, it is an intestinal toxin for sensitive insects such as G. mellonella [ 86 ]. The mode of action of this toxin can be evaluated further using insect model systems, for example, on G. mellonella larvae and Sf9 cells.…”

Entomotoxic Activity of the Extracts from the Fungus, <em>Alternaria tenuissima</em> and Its Major Metabolite, Tenuazonic Acid

“…The most well-known mechanisms of action of insecticidal and acaricidal compounds are malfunction of nervous system, blocking of postsynaptic receptors, inhibition of respiration, and developmental disorders [86]. The absence of considerable behavior and developmental changes, the lack of tremor, the weak sensitivity of sucking phytophages as well as an obvious antifeedant effect may indicate TeA is not an inhibitor of lipid biosynthesis like spirotetramat, but the intestinal toxin for sensitive insects [86]. From other hand, decreased viability and fertility of arthropods can also be achieved by the indirect action of TeA -by suppressing their symbiotic microflora and humoral immunity, as well as deterioration in the feed quality of the substrate [1].…”

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“…В обзоре П. Джешке «Состояние и перспективы открытия акарицидов и инсектицидов» (Jeschke, 2021) описан механизм действия брофланилида. Брофланилид, классифицируется как негативный аллостерический модулятор (NAM) рецепторов γ-аминомасляной кислоты (ГАМК) насекомых, поскольку дезметилброфланилид (DMBF) аллостерически ингибирует ГАМК-индуцированные ответы.…”