Two series of N-pyridylpyrazolecarboxamide derivatives were designed and synthesized by introducing D-alanine acid esters and D-serine acid esters into the skelecton of chlorantraniliprole. The obtained structures wer...Two series of N-pyridylpyrazolecarboxamide derivatives were designed and synthesized by introducing D-alanine acid esters and D-serine acid esters into the skelecton of chlorantraniliprole. The obtained structures were characterized by 1H NMR, 13C NMR, elemental analysis and specific optical rotation analysis. Preliminary bioas-says indicated that some compounds displayed excellent insecticidal activities against Mythimna separate and Plutella xylostella in comparison with chlorantraniliprole. In particular, IIq showed excellent insecticidal activity against Plutella xylostella with a mortality rate of 90% at 0.01 mg·L^-1. A 3D-QSAR （CoMSIA） study was per- formed in order to disclose the insecticidal structure-activity relationship and indicate the future work. The CoMS1A study demonstrated that large substitutes and electron deficient groups at the 3-position of pyrazole ring are favora- ble, the same as a small group near the ester groups of amino acid.展开更多
文摘Two series of N-pyridylpyrazolecarboxamide derivatives were designed and synthesized by introducing D-alanine acid esters and D-serine acid esters into the skelecton of chlorantraniliprole. The obtained structures were characterized by 1H NMR, 13C NMR, elemental analysis and specific optical rotation analysis. Preliminary bioas-says indicated that some compounds displayed excellent insecticidal activities against Mythimna separate and Plutella xylostella in comparison with chlorantraniliprole. In particular, IIq showed excellent insecticidal activity against Plutella xylostella with a mortality rate of 90% at 0.01 mg·L^-1. A 3D-QSAR （CoMSIA） study was per- formed in order to disclose the insecticidal structure-activity relationship and indicate the future work. The CoMS1A study demonstrated that large substitutes and electron deficient groups at the 3-position of pyrazole ring are favora- ble, the same as a small group near the ester groups of amino acid.
