title: Design of novel CSA analogues as potential safeners and fungicides.
abstract: 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.
authors.affiliation: Marine College, Shandong University at Weihai, No. 180, Wenhua West Road, Weihai 264209, PR China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Zheng
authors.affiliation: State Key Laboratory of Elemento-Organic Chemistry, Nankai University, No. 94 Weijin Road, Nankai District, Tianjin 300071, PR China.
authors.forename: Bin
authors.initials: B
authors.lastname: Liu
authors.affiliation: Marine College, Shandong University at Weihai, No. 180, Wenhua West Road, Weihai 264209, PR China.
authors.forename: Zhaopin
authors.initials: Z
authors.lastname: Gou
authors.affiliation: Marine College, Shandong University at Weihai, No. 180, Wenhua West Road, Weihai 264209, PR China.
authors.forename: Yao
authors.initials: Y
authors.lastname: Li
authors.affiliation: State Key Laboratory of Elemento-Organic Chemistry, Nankai University, No. 94 Weijin Road, Nankai District, Tianjin 300071, PR China.
authors.forename: Xiao
authors.initials: X
authors.lastname: Zhang
authors.affiliation: Marine College, Shandong University at Weihai, No. 180, Wenhua West Road, Weihai 264209, PR China.
authors.forename: Yanqing
authors.initials: Y
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Elemento-Organic Chemistry, Nankai University, No. 94 Weijin Road, Nankai District, Tianjin 300071, PR China.
authors.forename: Shujing
authors.initials: S
authors.lastname: Yu
authors.affiliation: State Key Laboratory of Elemento-Organic Chemistry, Nankai University, No. 94 Weijin Road, Nankai District, Tianjin 300071, PR China. Electronic address: bioassay@nankai.edu.cn.
authors.forename: Yonghong
authors.initials: Y
authors.lastname: Li
authors.affiliation: Marine College, Shandong University at Weihai, No. 180, Wenhua West Road, Weihai 264209, PR China. Electronic address: dequn.sun@sdu.edu.cn.
authors.forename: Dequn
authors.initials: D
authors.lastname: Sun
mesh_terms: D000935:Antifungal Agents / Q000737:chemistry* / Q000494:pharmacology; D015195:Drug Design; D005659:Fungicides, Industrial / Q000737:chemistry*; D006540:Herbicides / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000935:Antifungal Agents; D005659:Fungicides, Industrial; D006540:Herbicides
keywords: Antifungal activity; CSA analogues; Herbicide safeners; SAR; Synthesis