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Synthesis and insecticidal activity study of novel anthranilic diamides analogs containing a diacylhydrazine bridge as effective Ca2+ modulators.

Yunyun ZhouWei WeiLiangliang ZhuYuxin LiZhengming Li
Published in: Chemical biology & drug design (2018)
Anthranilic diamides is a class of insecticides target at ryanodine receptors (RyRs). To discover potent insecticides targeting at RyRs, a series of novel anthranilic diamides with a diacylhydrazine bridge were designed and synthesized. Their insecticidal activities were evaluated and a preliminary structure-activity relationship (SAR) was summarized. In particular, compound 5g exhibited good lethality against oriental armyworm (Mythimna separata) at a concentration of 5 mg/L. The calcium imaging experimental results indicated that the compound 5g can serve as effective insect Ca2+ level modulators by disrupting the cellular calcium homeostasis in Mythimna separata (Walker) and Spodoptera exigua (Hübner), which probably activated the RyRs on the ER membrane.
Keyphrases
  • structure activity relationship
  • aedes aegypti
  • small molecule
  • high resolution
  • molecular docking
  • protein kinase
  • cancer therapy
  • drug delivery
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  • estrogen receptor