Pro-insecticidal approach towards increasing in planta activity

Autor: Lawrence C, Creemer, Natalie C, Giampietro, William, Lambert, Maurice C, Yap, Gerrit J, deBoer, Yelena, Adelfinskaya, Scott, Castetter, Frank J, Wessels
Rok vydání: 2016
Předmět:
Zdroj: Pest management science. 73(4)
ISSN: 1526-4998
Popis: The adrenergic mode of action was investigated for the development of potential new insecticides. Clonidine-related analogs were tested against Myzus persicae (Sulzer) and Bemisia tabaci (Gennadius). Clonidine analogs lack translation owing to a possible vacuole-trapping mechanism. Physical property modulation via a prodrug approach was attempted to overcome this mechanism.Clonidine showed insecticidal activity against M. persicae and B. tabaci. A prodrug of a known open-chain analog of clonidine was developed. While the prodrug had decreased pKAdrenergic 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.
Databáze: OpenAIRE