微波促进的系统 xc-转运体抑制剂异噁唑酰肼的合成：初步同源建模。
Microwave accelerated synthesis of isoxazole hydrazide inhibitors of the system xc- transporter: Initial homology model.
机构信息
Department of Biomedical & Pharmaceutical Sciences, Center for Structural & Functional Neuroscience, The University of Montana, Missoula, MT 59812, United States; Medicinal Chemistry Graduate Program, The University of Montana, Missoula, MT 59812, United States.
出版信息
Bioorg Med Chem Lett. 2013 Nov 1;23(21):5931-5. doi: 10.1016/j.bmcl.2013.08.080. Epub 2013 Aug 27.
Abstract
Microwave accelerated reaction system (MARS) technology provided a good method to obtain selective and open isoxazole ligands that bind to and inhibit the Sxc- antiporter. The MARS provided numerous advantages, including: shorter time, better yield and higher purity of the product. Of the newly synthesized series of isoxazoles the salicyl hydrazide 6 exhibited the highest level of inhibitory activity in the transport assay. A homology model has been developed to summarize the SAR results to date, and provide a working hypothesis for future studies.
摘要
微波加速反应系统（MARS）技术为获得选择性和开放的异恶唑配体提供了一种很好的方法，这些配体可以结合并抑制 Sxc- 外排泵。MARS 具有许多优点，包括：反应时间更短、产物收率更高、纯度更高。在所合成的一系列异恶唑中，水杨酰肼 6 在转运实验中表现出最高的抑制活性。已经建立了一个同源模型来总结迄今为止的 SAR 结果，并为未来的研究提供一个工作假设。
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