Structure Simplification of Natural Products as a Lead Generation Approach in Agrochemical Discovery

Abstract

Natural products (NPs) have a long history as sources of compounds for crop protection. Perhaps a more important role for NPs has been as models and inspiration for the discovery and development of synthetic crop protection compounds. NPs and their synthetic mimics account for 18% of all crop protection compounds, whereas another 38% of all crop protection compounds have a NP that could have served as a model. Because NPs are often complex molecules, have limited availability, or possess structural features that constrain their suitability for use in agricultural settings, a key element in NP-inspired compounds is the simplification of the NP structure to provide a synthetically accessible molecule that possesses the physicochemical properties needed for use in crop protection. Herein we review a series of examples of NP mimics that demonstrate the structural or synthetic simplification of NPs as a guide for the discovery of future NP-inspired agrochemicals focused on fungicides, herbicides, and insecticides.

Antiviral Activities of Novel Myricetin Derivatives Containing 1,3,4‐Oxadiazole Bisthioether

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“…A micro thermophoresis instrument was used to research the interaction between TMV-CP and the compounds (NanoTemper Technologies GmbH, Germany). A 400 NMR spectrometer was used to obtain 1 H, 13 C and 19 F NMR spectra (Bruker Optics, Switzerland). The X-4B melting point instrument was used to obtain melting point data (Shanghai INESA Co., Ltd.).…”

“…The detailed 1 H, 13 C, 19 F-NMR and HR-MS characterization data of target compounds E1 -E20 was included in the Supporting Information. The representative data of E1 was exemplified.…”

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“…Natural products have been a source of new chemistries and new MOAs for pesticides, including herbicides 50,51 . Of commercial herbicides, natural products, modified natural products (e.g.…”