Pro‐insecticidal approach towards increasing in planta activity

Abstract

Adrenergic active compounds, such as clonidine analogs, show potential as insecticides; however, a designed prodrug approach did not overcome the lack of translation in this case. Studies confirmed that the synthesized prodrug analog metabolized in planta to the proposed vacuole-trapped compound. One possible explanation for the failure of this approach is that the rate of metabolism and vacuole trapping is faster than translaminar flow, and therefore the released pesticide is not biologically available to the target organism. © 2016 Society of Chemical Industry.

How To Design for a Tailored Subcellular Distribution of Systemic Agrochemicals in Plant Tissues

“…The present study aims to provide experimental evidence for the postulated vacuole trapping of basic pesticides in leaf cells. 10,11,34 The accumulation of weakly basic compounds in acidic organelles has been observed in animal and human cells 12,17,46,51 and was also recently discovered for acidic vesicles of protozoa. 20 Ion trapping of weakly acidic herbicides leads to phloem transport and systemic translocation in plants 27,48 and is well described for phytohormones such as auxins 21,35 and abscisic acid.…”

“…The present study aims to provide experimental evidence for the postulated vacuole trapping of basic pesticides in leaf cells. ,, …”

Innovations in Agrochemical Discovery and the Role of Metabolism, Bioavailability and Formulations

“…Finally, Creemer et al (Dow AgroSciences) describe their pro‐insecticide approach to delivering insecticidal activity. This connects thematically to the perspective articles, in that metabolism in plants and insects can play a significant role in achieving robust insecticidal activity or limiting it.…”