Design, synthesis and structure-activity relationship of novel diphenylamine derivatives

作者：Li Huichao; Guan Aiying; Huang Guang; Liu Chang Ling^*; Li Zhinian; Xie Yong; Lan Jie

来源：Bioorganic & Medicinal Chemistry, 2016, 24(3): 453-461.

DOI：10.1016/j.bmc.2015.09.032

• Diphenylamine derivatives
• Intermediate Derivatization Methods
• Fungicidal activity
• Structure-activity relationship

Diphenylamine derivatives have been reported with good fungicidal, insecticidal, acaricidal, rodenticidal and/or herbicidal activities. To find new lead compound of this kind, a series of novel diphenylamine derivatives were designed and synthesized by the approach of Intermediate Derivatization Methods. All compounds were identified by H-1 NMR and elemental analysis. Bioassays demonstrated that some compounds substituted at 2,4,6-positions or 2,4,5-positions of phenyl ring B exhibited excellent fungicidal activities. The optimal compounds P30 and P33 showed 80% and 85% control respectively against cucumber downy mildew at 12.5 mg L-1, both 100% control against rice blast at 0.3 mg L-1 and both 100% control against cucumber gray mold at 0.9 mg L-1. The relationship between structure and fungicidal activities was discussed as well.

• 出版日期2016-2-1
• 单位沈阳化工研究院有限公司