99988-56-4Relevant articles and documents
Toad Alkaloid for Pesticide Discovery: Dehydrobufotenine Derivatives as Novel Agents against Plant Virus and Fungi
Tian, Zhaoyong,Liao, Ancai,Kang, Jin,Gao, Yongyue,Lu, Aidang,Wang, Ziwen,Wang, Qingmin
, p. 9754 - 9763 (2021)
Plant viruses and fungi are a serious threat to food security and natural ecosystems. The efficient and environment-friendly control methods are urgently needed to help safeguard such resources. Here, we achieved the efficient synthesis of toad alkaloid dehydrobufotenine in eight steps with an overall yield of 8% from 5-methoxyindole. A series of dehydrobufotenine derivatives were designed, synthesized, and evaluated for their antiviral and fungicidal activities systematically. It was found for the first time that these compounds have good anti-plant virus activities and anti-plant pathogen activities. The antiviral activities of 21 compounds were similar to or better than those of ribavirin. Compounds 12 and 17 displayed better antiviral activities than ningnanmycin which is perhaps the most effective anti-plant virus agent. The antiviral mechanism research study of 12 revealed that it could make 20S CP disk fusion and aggregation. Further molecular docking results showed that there are hydrogen bonds between compounds 12, 17, and tobacco mosaic virus CP. The docking results are consistent with the antiviral activity. These compounds also displayed broad-spectrum fungicidal activities against 14 kinds of fungi, especially for Sclerotinia sclerotiorum. In this work, the synthesis, structure optimization, structure-activity relationship studies, and mode of action research of dehydrobufotenine alkaloids were carried out. It provides a reference for the development of the anti-plant virus agent and anti-plant pathogen agent from toad alkaloids.
3 - (1, 2, 4 - triazole [4, 3 - a] pyridine - 3 - yl) - 4 - (1H - Indol - 3 - yl) maleimide derivatives and its preparation method and application
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Paragraph 0035; 0036; 0051; 0052, (2017/08/25)
The invention provides a 3-(1,2,4-triazolo(4,3-a)pyridine-3-yl)-4-(1H-indole-3-yl)maleimide derivative with a novel structure and a preparation method and application of the derivative. The compound can be used for treating ischemic cerebral apoplexy. The general structural formula of the compound is shown in the specification.
Synthesis and biological evaluation of 3-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-4-(indol-3-yl)-maleimides as potent, selective GSK-3β inhibitors and neuroprotective agents
Ye, Qing,Mao, Weili,Zhou, Yubo,Xu, Lei,Li, Qiu,Gao, Yuanxue,Wang, Jing,Li, Chenhui,Xu, Yazhou,Xu, Yuan,Liao, Hong,Zhang, Luyong,Gao, Jianrong,Li, Jia,Pang, Tao
, p. 1179 - 1188 (2015/03/04)
A series of novel 3-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-4-(indol-3-yl)-maleimides were designed, prepared and evaluated for their GSK-3β inhibitory activities. Most compounds showed high potency to GSK-3β inhibition with high selectivity. Among them, compounds 7c, 7f, 7h, 7l and 7m significantly reduced GSK-3β substrate Tau phosphorylation at Ser396 in primary neurons, showing the inhibition of cellular GSK-3β. In the in vitro neuronal injury models, compounds 7c, 7f, 7h, 7l and 7m prevented neuronal death against glutamate, oxygen-glucose deprivation and nutrient serum deprivation which are associated with cerebral ischemic stroke. In the in vivo cerebral ischemia animal model, compound 7f reduced infarct size by 15% and improved the neurological deficit following focal cerebral ischemia. These findings may provide new insights into the development of novel GSK-3β inhibitors with potential neuroprotective activity.
