title: Design, synthesis and fungicidal activities of some novel pyrazole derivatives.
abstract: In order to discover new compounds with good fungicidal activities, 32 pyrazole derivatives were designed and synthesized. The structures of the target compounds were confirmed by 1H-NMR, 13C-NMR, and high-resolution electrospray ionization mass spectrometry (HR-ESI-MS), and their fungicidal activities against Botrytis cinerea, Rhizoctonia solani Kuhn, Valsa mali Miyabe et Yamada, Thanatephorus cucumeris (Frank) Donk, Fusarium oxysporum (S-chl) f.sp. cucumerinum Owen, and Fusarium graminearum Schw were tested. The bioassay results indicated that most of the derivatives exhibited considerable antifungal activities, especially compound 26 containing a p-trifluoromethyl- phenyl moiety showed the highest activity, with EC50 values of 2.432, 2.182, 1.787, 1.638, 6.986, and 6.043 μg/mL against B. cinerea, R. solani, V. mali, T. cucumeris, F. oxysporum, and F. graminearum, respectively. Moreover, the activities of compounds such as compounds 27-32 were enhanced by introducing isothiocyanate and carboxamide moieties to the 5-position of the pyrazole ring.
authors.affiliation: Research & Development Center of Biorational Pesticide, Key Laboratory of Plant Protection Resources and Pest Management of Ministry of Education, Northwest A&F University, Xinong Road 22, Yangling 712100, Shaanxi, China. xueruliu@nwsuaf.edu.cn.
authors.forename: Xue-Ru
authors.initials: XR
authors.lastname: Liu
authors.affiliation: Research & Development Center of Biorational Pesticide, Key Laboratory of Plant Protection Resources and Pest Management of Ministry of Education, Northwest A&F University, Xinong Road 22, Yangling 712100, Shaanxi, China. wgf20102010@nwsuaf.edu.cn.
authors.forename: Hua
authors.initials: H
authors.lastname: Wu
authors.affiliation: Research & Development Center of Biorational Pesticide, Key Laboratory of Plant Protection Resources and Pest Management of Ministry of Education, Northwest A&F University, Xinong Road 22, Yangling 712100, Shaanxi, China. skyhugh2012@gmail.com.
authors.forename: Ze-Yu
authors.initials: ZY
authors.lastname: He
authors.affiliation: Research & Development Center of Biorational Pesticide, Key Laboratory of Plant Protection Resources and Pest Management of Ministry of Education, Northwest A&F University, Xinong Road 22, Yangling 712100, Shaanxi, China. zhiqingma@nwsuaf.edu.cn.
authors.forename: Zhi-Qing
authors.initials: ZQ
authors.lastname: Ma
authors.affiliation: Research & Development Center of Biorational Pesticide, Key Laboratory of Plant Protection Resources and Pest Management of Ministry of Education, Northwest A&F University, Xinong Road 22, Yangling 712100, Shaanxi, China. fengjt@nwsuaf.edu.cn.
authors.forename: Jun-Tao
authors.initials: JT
authors.lastname: Feng
authors.affiliation: Research & Development Center of Biorational Pesticide, Key Laboratory of Plant Protection Resources and Pest Management of Ministry of Education, Northwest A&F University, Xinong Road 22, Yangling 712100, Shaanxi, China. zhxing1952@126.com.
authors.forename: Xing
authors.initials: X
authors.lastname: Zhang
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D005658:Fungi / Q000187:drug effects / Q000472:pathogenicity; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D021241:Spectrometry, Mass, Electrospray Ionization; D013329:Structure-Activity Relationship
chemical_list: D000935:Antifungal Agents; D011720:Pyrazoles; C031280:pyrazole