Synthesis, Bioactivities and Structure Activity Relationship of N-4-Methyl-1,2,3-thiadiazole-5-carbonyl-N′-phenyl Ureas (pages 2522–2532)
Dandan Guo, Zhiwen Wang, Zhijin Fan, Hui Zhao, Wei Zhang, Jiagao Cheng, Jiaqiang Yang, Qingjun Wu, Youjun Zhang and Qian Fan
Article first published online: 23 OCT 2012 | DOI: 10.1002/cjoc.201200268
29 novel N-4-methyl-1,2,3-thiadiazole-5-carbonyl-N′-phenyl ureas were designed and synthesized. Target compounds exhibit insecticidal activities. Bioassays indicated that compounds V-24 and V-22 exhibit outstanding insecticidal activity against Culex pipiens pallens and Plutella xylostella, respectively. Compound V-11 also has a broad-spectrum of fungicide activity against all the fungi tested. Five compounds show good SAR-inducing activity as well. These results establish basis for both disease and insect control in agricultural practice and novel pesticide development. Structure-activity relationship studies reveal that, with the contour maps based on steric and electrostatic CoMFA coefficients, we can conclude the relationship between the structures and bioactivity and continue the further design of highly active compounds.