- Discovery of Novel Benzo[4,5]thiazolo(oxazolo)[3,2-a]pyrimidinone Mesoionic Derivatives as Potential Antibacterial Agents and Mechanism Research
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A series of benzo[4,5]thiazole(oxazole)[3,2-a]pyrimidine mesoionic compounds were designed and synthesized. Antibacterial activity tests revealed that compound A23 showed good in vitro activities against Xanthomonas oryzae pv. Oryzicola (Xoc) and Xanthomo
- Liu, Ting,Shi, Jing,Liu, Dengyue,Zhang, Desheng,Song, Baoan,Hu, Deyu
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- Synthesis of NVS-BPTF-1 and evaluation of its biological activity
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BPTF (bromodomain and PHD finger containing transcription factor) is a multidomain protein that plays essential roles in transcriptional regulation, T-cell homeostasis and stem cell pluripotency. As part of the chromatin remodeling complex hNURF (nucleoso
- Mélin, Léa,Calosing, Cyrus,Kharenko, Olesya A.,Hansen, Henrik C.,Gagnon, Alexandre
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supporting information
(2021/07/10)
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- First Discovery of Novel Pyrido[1,2- a]pyrimidinone Mesoionic Compounds as Antibacterial Agents
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Plant bacterial diseases cause tremendous decreases in crop yield and quality, and there is a lack of highly effective and low-risk antibacterial agents. A series of novel pyrido[1,2-a]pyrimidinone mesoionic compounds containing vanillin moieties were synthesized, and the application of these mesoionic compounds as plant antibacterial agents was reported here for the first time. The bioassay results revealed that the mesoionic compounds had good antibacterial activity. Of these compounds, compound 11 showed excellent in vitro activity against Xanthomonas oryzae pv. oryzae, with an EC50 value of 1.1 μg/mL, which was substantially better than that of bismerthiazol (92.7 μg/mL) and thiodiazole copper (105.4 μg/mL). Moreover, greenhouse condition trials indicated that the protective and curative activities of compound 11 against rice bacterial leaf blight were 75.12 and 72.04%, respectively, which were better than those of bismerthiazol (62.24 and 50.83%, respectively) and thiodiazole copper (53.35 and 65.04%, respectively). These results provide a basis for the application of mesoionic vanillin moieties as new antibacterial agents.
- Liu, Dengyue,Zhang, Jian,Zhao, Lei,He, Wengjing,Liu, Zhengjun,Gan, Xiuhai,Song, Baoan
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- 3-methyl pyridino-[1,2-a] pyrimidone derivative containing 1-((4-benzyl-substituted)oxygroup) and application
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The invention discloses a 3-methyl pyridino-[1,2-a] pyrimidone derivative containing 1-((4-benzyl-substituted)oxygroup) and application. The general formula of the derivative is shown in the description, wherein R1 is a methoxyl group or an oxyethyl group or halogen; R2 is hydroxyl or isobutyl or ethyl or propyl or chloroethyl or 2-methoxyl group benzyl or 2-methoxyl group benzy or 2-fluorine benzyl or 2-cyanogroup benzyl chloride or 4-cyanogroup benzyl2-methyl benzyl chloride or 3-methyl benzyl chloride or 4-methyl benzyl chloride. According to the derivative, the rice bacterial leaf blight and citrus canker can be prevented and treated. The general formula is shown in the description.
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Paragraph 0055-0056
(2019/04/30)
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