Phenazine-1-carboxylic acid derivatives: Design, synthesis and biological evaluation against Rhizoctonia solani Kuhn

• Published in: Bioorganic & medicinal chemistry letters Vol. 20; no. 24; pp. 7369 - 7371
• Main Authors: Ye, Long, Zhang, Hongyan, Xu, Hong, Zou, Qi, Cheng, Chao, Dong, Dexian, Xu, Yuquan, Li, Rongxiu
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier Ltd 15.12.2010; Elsevier
• Subjects: Antifungal activity; Antifungal Agents - chemical synthesis; Antifungal Agents - chemistry; Antifungal Agents - pharmacology; Biological and medical sciences; Chemical control; Control; Drug Design; Fundamental and applied biological sciences. Psychology; Fungal plant pathogens; Oryza sativa; Phenazine-1-carboxylic acid; Phenazines - chemical synthesis; Phenazines - chemistry; Phenazines - pharmacology; Phytopathology. Animal pests. Plant and forest protection; Rhizoctonia - drug effects; Rhizoctonia solani; Rhizoctonia solani Kuhn; Rice; Sheath blight; Structure-Activity Relationship; Antifungal activity; Sheath blight; Phenazine-1-carboxylic acid; Rhizoctonia solani Kuhn; Rice; Plant pathogen; Pesticides; Biological activity; Fungicide; Fungi; Phenazine derivatives; Carboxamide; Rhizoctonia solani; Fungi Imperfecti; Chemical synthesis
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2010.10.050

Rhizoctonia solani Kuhn is the pathogen that causes sheath blight and results in significant yield reduction in rice and in nearly 50 other crops. In order to develop a new fungicide effective against this pathogen, a series of structurally diverse phenazine-1-carboxylic acid derivatives, 2a, 2b, 2c, 2d, 2e, 2f, 2g, 2h, 2i, 2j, and 2k, were designed, synthesized and evaluated for their antifungal activity. The two most active compounds 2i and 2j were selected as lead compounds for further antifungal research. Rhizoctonia solani Kuhn is the pathogen that causes sheath blight and results in significant yield reduction in rice and in nearly 50 other crops. In order to develop a new fungicide effective against this pathogen, a series of structurally diverse phenazine-1-carboxylic acid derivatives, 2a, 2b, 2c, 2d, 2e, 2f, 2g, 2h, 2i, 2j, and 2k, were designed, synthesized and evaluated for their antifungal activity. The two most active compounds 2i and 2j were selected as lead compounds for further antifungal research.