Design,synthesis and antifungal evaluation of novel pyrazole carboxamides with diarylamines scaffold as potent succinate dehydrogenase inhibitors |
| |
Authors: | Aigui Zhang Jingya Zhou Ke Tao Taiping Hou Hong Jin |
| |
Institution: | Key Laboratory of Bio-Resource and Eco-Environment of Ministry of Education, College of Life Sciences, Sichuan University, Chengdu 610065, Sichuan, PR China |
| |
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. |
| |
Keywords: | Pyrazole carboxamides Synthesis Succinate dehydrogenase inhibitors Antifungal activities |
本文献已被 ScienceDirect 等数据库收录! |
|