期刊
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
卷 62, 期 18, 页码 4063-4071出版社
AMER CHEMICAL SOC
DOI: 10.1021/jf405437k
关键词
nicotinamide; antifungal activity; succinate dehydrogenase inhibitors
资金
- National Basic Research Program of China [2010CB126100]
- National Natural Science Foundation of China [30901854]
- Fundamental Research Funds for the Central Universities [KYZ201107]
- Special Fund for Agro-scientific Research in the Public Interest [201303023]
Thirty-eight nicotinamide derivatives were designed and synthesized as potential succinate dehydrogenase inhibitors (SDHI) and precisely characterized by H-1 NMR, ESI-MS, and elemental analysis. The compounds were evaluated against two phytopathogenic fungi, Rhizoctonia solani and Sclerotinia sclerotiorum, by mycelia growth inhibition assay in vitro. Most of the compounds displayed moderate activity, in which, 3a-17 exhibited the most potent antifungal activity against R. solani and S. sclerotiorum with IC50 values of 15.8 and 20.3 mu M, respectively, comparable to those of the commonly used fungicides boscalid and carbendazim. The structure-activity relationship (SAR) of nicotinamide derivatives demonstrated that the meta-position of aniline was a key position contributing to the antifungal activity. Inhibition activities against two fungal SDHs were tested and achieved the same tendency with the data acquired from in vitro antifungal assay. Significantly, 3a-17 was demonstrated to successfully suppress disease development in S. sclerotiorum infected cole in vivo. In the molecular docking simulation, sulfur and chlorine of 3a-17 were bound with PHE291 and PRO150 of the SDH homology model, respectively, which could explain the probable mechanism of action between the inhibitory and target protein.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据