Literature DB >> 30097371

Design, synthesis and antifungal evaluation of novel pyrazole carboxamides with diarylamines scaffold as potent succinate dehydrogenase inhibitors.

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.
Copyright © 2018 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Antifungal activities; Pyrazole carboxamides; Succinate dehydrogenase inhibitors; Synthesis

Mesh:

Substances:

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


  4 in total

1.  A novel series of pyrazole derivatives toward biological applications: experimental and conceptual DFT characterization.

Authors:  Pedro D Ortiz; Judith Castillo-Rodriguez; Jorge Tapia; Ximena Zarate; Gabriel A Vallejos; Vanesa Roa; Elies Molins; Carlos Bustos; Eduardo Schott
Journal:  Mol Divers       Date:  2021-11-01       Impact factor: 3.364

2.  1,2,4-Oxadiazole-Based Bio-Isosteres of Benzamides: Synthesis, Biological Activity and Toxicity to Zebrafish Embryo.

Authors:  Sen Yang; Chao-Li Ren; Tian-Yang Ma; Wen-Qian Zou; Li Dai; Xiao-Yu Tian; Xing-Hai Liu; Cheng-Xia Tan
Journal:  Int J Mol Sci       Date:  2021-02-27       Impact factor: 5.923

3.  Design, Synthesis and Antifungal/Nematicidal Activity of Novel 1,2,4-Oxadiazole Derivatives Containing Amide Fragments.

Authors:  Dan Liu; Ling Luo; Zhengxing Wang; Xiaoyun Ma; Xiuhai Gan
Journal:  Int J Mol Sci       Date:  2022-01-29       Impact factor: 5.923

4.  Synthesis and Biological Evaluation of Novel Benodanil-Heterocyclic Carboxamide Hybrids as a Potential Succinate Dehydrogenase Inhibitors.

Authors:  Jian Yang; Yongtian Zhao; Jun Wan; Mingfang Jiang; Hong Jin; Ke Tao; Taiping Hou
Journal:  Molecules       Date:  2020-09-18       Impact factor: 4.411

  4 in total

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