- A novel benzoyl pyrimidine urea compound and its preparation and use (by machine translation)
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The invention provides a benzoyl pyrimidine urea compound, of formula I or formula II structure shown. The present invention provides benzoyl pyrimidine urea compound has excellent armyworm killing, mosquito killing and broad-spectrum antifungal activity. The experimental result shows, the present invention provides benzoyl pyrimidine urea compound in 0.5 μg mL- 1 Sliding surface of larvae activity can be up to 100%, in the 0.25μg mL- 1 Sliding surface of larvae activity can be up to 100%. In the 50 μg mL- 1 When, demonstrated broad-spectrum antifungal activity, and to the cabbage in vitro blade has a certain protective effect. And low toxicity to fish, LC to the zebra fish50 Are respectively 378.387 mg L- 1 , 21.668 Mg L- 1 . Can be used to prepare insecticidal, anti-plant-pathogenic fungi pesticide application. (by machine translation)
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Paragraph 0095; 0096; 0097; 0099; 0101
(2019/01/06)
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- Investigation of novel pesticides with insecticidal and antifungal activities: Design, synthesis and SAR studies of benzoylpyrimidinylurea derivatives
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In order to find pesticides with insecticidal and antifungal activities, a series of novel benzoyl pyrimidinylurea derivatives were designed and synthesized. All target compounds were identified by 1H-NMR spectroscopy and HRMS. Insecticidal and antifungal activity of these compounds were evaluated and the structure-activity relationships (SAR) were clearly and comprehensively illustrated. Compound 7, with low toxicity to zebrafish (LC50 = 378.387 μg mL?1) showed 100% inhibition against mosquito (Culex pipiens pallens) at 0.25 μg mL?1. Both compounds 19 and 25 exhibited broad-spectrum fungicidal activity (>50% inhibitory activities against 13 phytopathogenic fungi), which were better than those of the commercial pesticide pyrimethanil (>50% inhibitory activities against eight phytopathogenic fungi). Furthermore, compounds 19 and 25 exhibited protective activity against Sclerotinia sclerotiorum on leaves of Brassica oleracea L. during in vivo experiments.
- Chen, Peiqi,Song, Xiangmin,Fan, Yongmei,Kong, Weihao,Zhang, Hao,Sun, Ranfeng
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- CHEMICAL COMPOUNDS
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The invention is directed to to substituted indazole derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1 - R6 and X are defined herein. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of disorders characterized by constitutively activated ACG kinases such as cancer and more specifically leukemia and cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
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Page/Page column 96
(2010/11/04)
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