期刊
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
卷 65, 期 5, 页码 1021-1029出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jafc.6b05134
关键词
succinate ubiquinone oxidoreductase; complex II; diphenyl ether; structure-activity relationship; molecular docking
资金
- National Key Technologies RD Program [2014BAD23B00]
- National Natural Science Foundation of China [21332004, 21272092]
A series of diphenyl ether-containing pyrazole-carboxamide derivatives was designed and synthesized as new succinate ubiquinone oxidoreductase (SQR) inhibitors. This highly potent molecular scaffold was developed from a moderately activie hit 3, obtained from our previous pharmacophore-linked fragment virtual screening (PFVS) method. The results of greenhouse tests indicated that some analogues showed good SQR inhibitory activity, with promising fungicidal activity against Rhizoctonia solani and Sphaerotheca fuliginea at a dosage of 200 mg/L. Most surprisingly, compound 62 showed the highest SQR inhibitory activity with a K-i value of 0.081 mu M, about 4-fold more potent than penthiopyrad (K-i = 0.307 mu W. In addition, compounds 43 and 62 displayed excellent fungicidal activity even at a dosage as low as 6.25 mg/L, which was superior to thifluzamide. Moreover, compound 62 exhibited excellent protection effect against R. solani and provided about 81.2% protective control efficancy after 21 days with two sprayings. The present work indicated that these two compounds could be used as potential agricultural fungicides targeting SQR.
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