Design, synthesis and bioactivity evaluation of novel acylthiourea derivatives of cantharidin.

摘要

In an attempt to find the biorational pesticides, a series of novel acylthiourea derivatives of cantharidin were designed, synthesized and preliminarily evaluated for their bioactivities against Tetranychus cinnabarinus and Brevicoryne brassicae. All the new compounds showed significant acaricidal activities against T. cinnabarinus with LC₅₀ values ranging from 0.695 to 2.934 mmol/L. In particular, compounds 6i and 6 g exhibited the greatest acaricidal activity against T. cinnabarinus in all derivatives we prepared. Moreover, all of these compounds displayed better acaricidal activities against T. cinnabarinus than insecticidal activities against B. brassicae. Based on the observed bioactivities, the structure-activity relationship (SAR) of these analogs was also discussed. The present work indicated that some cantharidin derivatives can be used as potential lead compounds for developing novel insecticides and acaricides.