4.5 Article

Synthesis and biological activities of novel 1,3,4-thiadiazole-containing pyrazole oxime derivatives

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 26, Issue 15, Pages 3818-3821

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.04.094

Keywords

1,3,4-Thiadiazole; Pyrazole oxime; Synthesis; Bioactivity

Funding

  1. National Natural Science Foundation of China [21202089, 21372135]
  2. Research Foundation of the Six People Peak of Jiangsu Province [2013-SWYY-013]
  3. Natural Science Foundation of Jiangsu Province [BK20140425]
  4. Technology Project Fund of Nantong City [AS2014011, CP12013002]

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A new library of 1,3,4-thiadiazole-containing pyrazole oximes was designed and synthesized. Their acaricidal and insecticidal activities were evaluated. Bioassay results indicated that some target compounds exhibited good acaricidal and insecticidal properties. Especially, compound 8m had 80% acaricidal activity against Tetranychus cinnabarinus at the concentration of 50 mu g/mL, compound 8f displayed 100% insecticidal activities against Aphis craccivora at the concentration of 50 mu g/mL, compounds 8r and 8w showed 100% insecticidal activities against Plutella xylostella at the concentration of 50 mu g/mL. Furthermore, compounds 8r (LC50 = 19.61 mu g/mL) and 8w (LC50 = 9.78 mu g/mL) possessed comparable or even better insecticidal activities than the control Pyridalyl (LC50 = 17.40 mu g/mL) against P. xylostella. (C) 2016 Elsevier Ltd. All rights reserved.

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