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Cercosporin-Photocatalyzed [4+1]- and [4+2]-Annulations of Azoalkenes Under Mild Conditions
Published on: July 17, 2020
Design, synthesis and bioactivity evaluation of novel benzophenone hydrazone derivatives
Wen-Qun Li1, Zhi-Jun Zhang, Xiang Nan
1School of Pharmacy, Lanzhou University, Lanzhou, 730000, People's Republic of China.
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 LC50 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 LC50 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.
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