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Design, synthesis and bioactivity evaluation of novel benzophenone hydrazone derivatives
Author(s) -
Li WenQun,
Zhang ZhiJun,
Nan Xiang,
Liu YingQian,
Hu GuanFang,
Yu HaiTao,
Zhao XiaoBo,
Wu Dan,
Yan LiTing
Publication year - 2014
Publication title -
pest management science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.296
H-Index - 125
eISSN - 1526-4998
pISSN - 1526-498X
DOI - 10.1002/ps.3607
Subject(s) - hydrazone , benzophenone , thiourea , chemistry , urea , molecule , chemical structure , combinatorial chemistry , stereochemistry , organic chemistry
BACKGROUND Benzophenone hydrazone derivatives are among the most important classes of synthetic insecticides. In an effort to discover new molecules with good insecticidal/acaricidal activities, a series of novel benzophenone hydrazone N ‐acylated thiourea and urea derivatives was synthesized and bioassayed . RESULTS All of these compounds exhibited excellent bioactivities against T. cinnabarinus and B. brassicae , especially towards T. cinnabarinus with LC 50 values ranging from 0.305 to 2.036 mmol L ‐1 . Moreover, the acaricidal activities against T. cinnabarinus of compounds 8a–i, 12b–f and 12h were 2.5–5.5‐fold that of parent molecule 3 based on the LC 50 value . CONCLUSION Based on the observed bioactivities, the structure–activity relationship of these analogs was also discussed. Structure–activity relationships provided information that could direct further investigation on structure modification. Our studies indicated that benzophenone hydrazone N ‐acylated thiourea and urea derivatives could be used as potential lead compounds for developing novel acaricides and insecticides. © 2013 Society of Chemical Industry

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