Comer Eamon, Duvall Jeremy R, duPont Lee Maurice
Therapeutics Platform, Broad Institute of MIT & Harvard, 7 Cambridge Center, Cambridge, MA 02142, USA.
Future Med Chem. 2014;6(17):1927-42. doi: 10.4155/fmc.14.111.
The development of resistance to existing antimicrobials has created a threat to human health that is not being addressed through our current drug pipeline. Limitations with the use of commercial vendor libraries and natural products have created a need for new types of small molecules to be screened in antimicrobial assays. Diversity oriented synthesis (DOS) is a strategy for the efficient generation of compound collections with a high degree of structural diversity. Diversity-oriented synthesis molecules occupy the middle ground of both complexity and efficiency of synthesis between natural products and commercial libraries. In this review we focus upon the use of diversity-oriented synthesis compound collections for the discovery of new antimicrobial agents.
对现有抗菌药物产生耐药性的情况对人类健康构成了威胁,而我们目前的药物研发渠道无法应对这一威胁。商业供应商文库和天然产物使用上的局限性,使得有必要在抗菌检测中筛选新型小分子。多样性导向合成(DOS)是一种有效生成具有高度结构多样性的化合物库的策略。多样性导向合成的分子在天然产物和商业文库之间占据了合成复杂性和效率的中间地带。在本综述中,我们重点关注利用多样性导向合成化合物库来发现新型抗菌剂。