Journal
CHINESE JOURNAL OF CHEMISTRY
Volume 30, Issue 10, Pages 2522-2532Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cjoc.201200268
Keywords
4-methyl-1; 2; 3-thiadiazole derivatives; benzoylurea pesticides; insecticidal activity; 3D QSAR model
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Funding
- National Natural Science Foundation of China [20872071]
- Tianjin Natural Science Foundation [10JCZDJC17500]
- National Key Project for Basic Research [2010CB126105]
- National Key Technology Research and Development Program [2011BAE06B02]
- Foundation of Achievements Transformation and Spreading of Tianjin Agricultural Science and Technology [201002250]
- Tianjin Key Technology Research and Development Program [11ZCGYNC00100]
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Twenty nine novel N-4-methyl-1,2,3-thiadiazole-5-carbonyl-N'-phenyl ureas were designed and synthesized, and their structures were confirmed by proton nuclear magnetic resonance (1H NMR), infra red spectroscopy (IR) and high-resolution mass spectroscopy (HRMS). Compounds V-9, V-11, V-12, V-15, V-19, V-21, V-22 and V-24 exhibit excellent activity against Culex pipiens pallens. Compounds V-12 and V-22 present good insecticidal activity against Plutella xylostella L. Their median lethal concentrations (LC50) are 164.15 and 89.69 mg center dot L-1, respectively. Compound V-11 also has potential wide spectrum of fungicide activity. Its median effective concentrations (EC50) detected from 3.82 mu g center dot mL-1 against Physalospora piricola to 31.60 mu g center dot mL-1 against Cercospora arachidicola. Compounds V-15 and V-24 show outstanding induction activities as same as positive controls TDL and ningnanmycin, furthermore V-24 has the highest induction activity of 41.85%+/- 4.43%. To elucidate the structure activity relationship in these compounds, a 3D-QSAR model has been built. The established model showed a reliable predicting ability with q2 values of 0.643 and r2 values of 0.982.
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