An azido-oxazolidinone antibiotic for live bacterial cell imaging and generation of antibiotic variants through Biotage Isolera耐士科技
2015-02-13 10:09
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The 3-aryl-2-cyanoacrylamide scaffold was designed as core pharmacophore for inhibitors of the Dengue and West Nile virus serine proteases (NS2B-NS3). A total of 86 analogs was prepared to study the structure–activity relationships in detail. Thereby, it turned out that the electron density of the aryl moiety and the central double bond have a crucial influence on the activity of the compounds, whereas the influence of substituents of the amide residue is less relevant. The para-hydroxy substituted analog was found
to be the most potent inhibitor in this series with a Ki-value of 35.7 lM at the Dengue and 44.6 lM at the West Nile virus protease. The aprotinin competition assay demonstrates a direct interaction of the inhibitor molecule with active centre of the Dengue virus protease. The target selectivity was studied in a counterscreen with thrombin and found to be 2.8:1 in favor of DEN protease and 2.3:1 in favor of WNV protease, respectively.
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We herein report several highly active catalyst systems with thiadiazolidine 1-oxides as ligands for palladium in the MizorokieHeck reaction. Excellent yields of stilbenes derived from aryl iodides and bromides have been achieved using as little as 0.00002 mol % catalyst. The ligand/palladiumsystem can be stored as a stock solution open to air at room temperature with no observable loss of activity for a period of several months.
耐士科技作为Biotage中国区总代理,以优质的服务为您提供Biotage全系产品以及相关的技术服务。1、开机前确认自动收集机械手臂下无障碍物,试管高度低于机械手臂收集针
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耐士科技作为Biotage中国区总代理,以优质的服务为您提供Biotage全系产品以及相关的技术服务。
操作步骤:
1.开机,按屏幕左下方黑色电源键
2.进入开机界面后,点击
Organic Synthesis
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