Department of Chemistry, University of British Columbia, 2036 Main Mall, Vancouver, BC, Canada.
Nat Prod Rep. 2010 Mar;27(3):330-42. doi: 10.1039/b919071f. Epub 2010 Jan 22.
Micrococcin P1, 1, is an antibiotic that exhibits noteworthy antibacterial, antiprotozoal, antimalarial,cytotoxic, and gene-modulating activities. This notwithstanding, its precise structure remained undefined until mid-2009, when our group carried out the total synthesis of a substance that proved to be spectroscopically and polarimetrically identical to the natural product. This work lifted all structural and stereochemical ambiguities that have surrounded micrococcin since its discovery. Of course,knowledge of the precise structure of the molecule is essential in understanding intimate details of its mode of action and in charting possible medicinal chemistry activity. This review summarizes present knowledge about the sources, properties, and chemical synthesis of micrococcin P1.
微球菌素 P1,1,是一种具有显著抗菌、抗原生动物、抗疟疾、细胞毒性和基因调节活性的抗生素。尽管如此,直到 2009 年年中,当我们的团队进行了一种物质的全合成,证明其在光谱和旋光性上与天然产物完全一致时,其确切结构仍然没有被定义。这项工作消除了自发现微球菌素以来一直存在的所有结构和立体化学上的不确定性。当然,对分子的精确结构的了解对于理解其作用模式的细微细节以及描绘可能的药物化学活性是至关重要的。这篇综述总结了目前关于微球菌素 P1 的来源、性质和化学合成的知识。