Novel amino acid ester-chlorantraniliprole conjugates: design, synthesis, phloem accumulation and bioactivity.

摘要: Background Conjugating amino acid and glucose fragments with existing pesticide structures has been shown to be an effective way introduce phloem mobility into non-phloem mobile species. However, the resulting derivatives always suffer from lower bioactivity compared their parent compound. To solve this problem, we designed synthesised a series of ester-capped amino-acid-conjugated chlorantraniliproles. Results The systemic test showed that all conjugates exhibited excellent xylem in Ricinus communis model. In particular, compounds 7b, 8b 8c were able accumulate tissues form hydrolysis products, concentrations sap can reach 3 times concentration incubation medium. Although insecticidal activity (LC50 ) against beet armyworm (Spodoptera exigua) vitro was weaker than chlorantraniliprole, similar vivo Conclusions This work provides potential strategy obtain possess both improved uptake crops while retaining effect © 2017 Society Chemical Industry.