Laboratory of Chemical Biology of Natural Products and Designed Molecules, Institute of Physical Chemistry, NCSR DEMOKRITOS, Athens, Greece.
Bioorg Med Chem Lett. 2010 Dec 15;20(24):7488-92. doi: 10.1016/j.bmcl.2010.10.001. Epub 2010 Oct 8.
Previous work from our group described the synthesis and biological evaluation of new rigid, 6,6- and 6,7-spiro aminoglycosidic scaffolds targeting the bacterial ribosome. Herein we describe an improved synthetic protocol for their construction, and extend our study by further amino-functionalization of their 6,7-spiro analogs. The synthetic strategy, preparation and evaluation of some representative examples are reported.
我们小组之前的工作描述了新的刚性、6,6-和 6,7-螺环氨基糖苷类骨架的合成和生物评价,这些骨架针对细菌核糖体。本文中我们描述了其构建的改进合成方案,并通过进一步对 6,7-螺环类似物进行氨基官能化来扩展我们的研究。报道了一些代表性实例的合成策略、制备和评价。