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Synthesis and Bio-activities of Pyrazolyl or Pyridinyl Substituted Tonghaosu Analogs
作者姓名:尹标林  陈立  徐汉虹  张健存  吴毓林
作者单位:[1]Guangzhou Institute of Biomedicine and Health, Chinese Academy of Science, Guangzhou, Guangong 510663, China [2]State Key Laboratory ofBio-organic & Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China [3]Laboratory of Insect Toxicology, South China Agricultural University, Guangzhou, Guangdong 510642, China
摘    要:11 pyrazolyl or pyridinyl substituted tonghaosu analogs were synthesized. Structures of all the new compounds were confirmed by ^1H NMR, IR, MS, HREIMS or elemental analysis. Their antifeedant activity against larvae of large white butterfly (Pieris brassicae L.), larvicidal activity toward mosquito (Culex quinquefasciatus Say) and growth control activity toward larvae of Spodoptera litura Fab were examined. Some of them exhibited antifeeding activities comparable to or stronger than tonghaosu Z-1. Based on the activity data, the preliminary structure-activity relationship was also discussed, which might be instructive for finding out lead compounds with better bioactivities in the future.

关 键 词:吡唑基取代茼蒿素类似物  吡啶取代茼蒿素类似物  合成  生物活性  拒食素  杀幼虫剂
修稿时间:2006-11-162007-02-27

Synthesis and Bio-activities of Pyrazolyl or Pyridinyl Substituted Tonghaosu Analogs
YIN, Biao-Lin CHEN, Li XU, Han-Hong ZHANG, Jian-Cun WU, Yu-Lin.Synthesis and Bio-activities of Pyrazolyl or Pyridinyl Substituted Tonghaosu Analogs[J].Chinese Journal of Chemistry,2007,25(6):808-813.
Authors:YIN  Biao-Lin CHEN  Li XU  Han-Hong ZHANG  Jian-Cun WU  Yu-Lin
Institution:[1]Guangzhou Institute of Biomedicine and Health, Chinese Academy of Science, Guangzhou, Guangong 510663, China; [2]State Key Laboratory ofBio-organic & Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China; [3]Laboratory of Insect Toxicology, South China Agricultural University, Guangzhou, Guangdong 510642, China
Abstract:11 pyrazolyl or pyridinyl substituted tonghaosu analogs were synthesized. Structures of all the new compounds were confirmed by 1H NMR, IR, MS, HREIMS or elemental analysis. Their antifeedant activity against larvae of large white butterfly (Pieris brassicae L.), larvicidal activity toward mosquito (Culex quinquefasciatus Say) and growth control activity toward larvae of Spodoptera litura Fab were examined. Some of them exhibited antifeeding activities comparable to or stronger than tonghaosu Z‐1 . Based on the activity data, the preliminary structure‐activity relationship was also discussed, which might be instructive for finding out lead compounds with better bioactivities in the future.
Keywords:spiroketal  tonghaosu analog  antifeedant  Larvicidal  growth control  Pieris brassicae  Culex quinquefasciatus  Spodoptera litura
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