| Literature DB >> 30097371 |
Aigui Zhang1, Jingya Zhou1, Ke Tao1, Taiping Hou1, Hong Jin2.
Abstract
Sixteen novel pyrazole carboxamides with diarylamines scaffold were designed, synthesized and characterized in detail via 1H NMR, 13C NMR and ESI-HRMS. Preliminary bioassays showed that some of the target compounds exhibited good antifungal activity against Rhizoctonia solani, Fusarium oxysporum, Phytophthora infestans and Fusarium graminearum. Among them, compound 1c exhibited the highest antifungal activities against R. solani in vitro with EC50 value of 0.005 mg/L, superior to the commercially available fungicide fluxapyroxad (EC50 = 0.033 mg/L). And compound 1c (IC50 = 0.034 mg/L) showed higher inhibition abilities against succinate dehydrogenase than fluxapyroxad (IC50 = 0.037 mg/L). This study suggests that compound 1c could be regarded as a potential succinate dehydrogenase inhibitor.Entities:
Keywords: Antifungal activities; Pyrazole carboxamides; Succinate dehydrogenase inhibitors; Synthesis
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Year: 2018 PMID: 30097371 DOI: 10.1016/j.bmcl.2018.08.001
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823