- Discovery of Pyrazine-Carboxamide-Diphenyl-Ethers as Novel Succinate Dehydrogenase Inhibitors via Fragment Recombination
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The discovery of novel succinate dehydrogenase inhibitors (SDHIs) has attracted great attention worldwide. Herein, a fragment recombination strategy was proposed to design new SDHIs by understanding the ligand-receptor interaction mechanism of SDHIs. Thre
- Li, Hua,Gao, Meng-Qi,Chen, Yan,Wang, Yu-Xia,Zhu, Xiao-Lei,Yang, Guang-Fu
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p. 14001 - 14008
(2020/11/27)
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- HETEROARYL RHEB INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same. Compositions comprising a compound of this invention or a pharmaceutically acceptable derivative thereof and a pharmaceutically acceptable carrier, adjuvant, or vehicle. The amount of the compound in compositions of this invention is such that it is effective to measurably inhibit Rheb, in a biological sample or in a patient.
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Paragraph 00585
(2018/11/10)
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- Pyrazinamide compounds and preparing method and application thereof and bactericide
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The invention relates to the field of pesticide bactericides, and discloses a pyrazinamide compound and a preparing method and application thereof and a bactericide. The pyrazinamide compound has thestructure shown in the formula (I) or the formula (II) or the formula (III). According to the pyrazinamide compound and the preparing method and application thereof and the bactericide, by introducingpyrazine ring fragments and and diphenyl ether fragments with the wide biological activity in NNF-0721, and the pyrazinamide compound with the brand-new structure is designed; the pyrazinamide compound can serve as a brand-new succinodehydrogenase inhibitor or a bactericide. The formula is defined in the description.
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Paragraph 0184; 0185; 0186; 0189
(2019/01/14)
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- Metal-free oxidative coupling: Xanthone formation via direct annulation of 2-aryloxybenzaldehyde using tetrabutylammonium bromide as a promoter in aqueous medium
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A metal-free intramolecular annulation of 2-aryloxybenzaldehydes to xanthones is disclosed, which proceeds through the direct oxidative coupling of an aldehyde C-H bond and aromatic C-H bonds using tetrabutylammonium bromide (TBAB) as a promoter in aqueous medium. This strategy works smoothly in the presence of both electron-donating and electron-withdrawing groups, and displays good tolerance towards catalytically reactive substituents, thus promising further functionalizations of xanthone products.
- Rao, Honghua,Ma, Xinyi,Liu, Qianzi,Li, Zhongfeng,Cao, Shengli,Li, Chao-Jun
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supporting information
p. 2191 - 2196
(2013/10/01)
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- 1-(2-Phenoxyphenyl)methanamines: SAR for dual serotonin/noradrenaline reuptake inhibition, metabolic stability and hERG affinity
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A novel series of 1-(2-phenoxyphenyl)methanamines is disclosed, which possess selective dual 5-HT and NA reuptake pharmacology. Analogues with good human in vitro metabolic stability, hERG selectivity and passive membrane permeability were identified.
- Whitlock, Gavin A.,Blagg, Julian,Fish, Paul V.
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p. 596 - 599
(2008/09/20)
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