Antifungal agents. Part 5: synthesis and antifungal activities of aminoguanidine derivatives of N-arylsulfonyl-3-acylindoles.
In order to discover more promising antifungal agents, a series of aminoguanidine derivatives of N-arylsulfonyl-3-acylindoles (5a-r) were prepared and evaluated in vitro for their antifungal activities against seven phytopathogenic fungi. Especially compounds 5n and 5o exhibited more potent antifungal activities than or comparable to hymexazol, a commercially available agricultural fungicide at the concentration of 100 μg/mL. Preliminary structure-activity relationships study demonstrated that introduction of electron-donating substituents R(1) and R(2), and the proper length of substituent R(3) were usually very important for their antifungal activities.
Laboratory of Pharmaceutical Design and Synthesis, College of Sciences, Northwest A&F University, Yangling, China. orgxuhui@nwsuaf.edu.cn
Hui
H
Xu
Yang-Yang
YY
Wang
D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D005658:Fungi / Q000187:drug effects; D006146:Guanidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D007211:Indoles / Q000737:chemistry*; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; D006146:Guanidines; D007211:Indoles; C004479:pimagedine