Design of novel CSA analogues as potential safeners and fungicides.

Study of safeners has been seldom reported in literature. In this work, a series of novel acylsulfamoylbenzamide analogues was designed and synthesized with newly developed safener cyprosulfamide (CSA) as the leading compound. The activity assay against the herbicide thiencarbazone-methyl (TCM) on maize revealed that fifteen compounds showed better protective effect than CSA on the fresh weight of aerial parts, twelve compounds exhibited better activity on the dry weight of aerial parts. Remarkably, two compounds (6Ih, 7II) had protective effect on the four aspects of TCM treated maize. Further antifungal assay showed their excellent activity against Physollospora piricola. The structure-activity relationships of CSA analogues as safeners and fungicides were discussed and it might be valuable for further molecular modification of new CSA analogues.

Diversity oriented design of various benzophenone derivatives and their in vitro antifungal and antibacterial activities.

A series of new substituted benzophenone derivatives was designed, synthesized and screened for their antifungal and antibacterial activities. The bioassays indicated that most of the synthesized compounds showed some antifungal activity against the tested phytopathogenic fungi, but lower antibacterial activities towards the five vibrios isolated from marine sources. The preliminary structure activity relationship (SAR) of the compounds was also discussed.