Department of Chemistry, Umeå University, SE-90187 Umeå, Sweden.
Molecules. 2010 Jun 21;15(6):4423-38. doi: 10.3390/molecules15064423.
Salicylidene acylhydrazides are inhibitors of type III secretion in several gram-negative pathogens. To further develop the salicylidene acylhydrazides, scaffold hopping was applied to replace the core fragment of the compounds. The novel 2-(2-amino-pyrimidine)-2,2-difluoroethanol scaffold was identified as a possible analog to the salicylidene acylhydrazide core structure. The synthesis of a library of 2-(2-amino-pyrimidine)-2,2-difluoro-ethanols is described in this paper.
水杨酰腙类化合物是几种革兰氏阴性病原体中 III 型分泌系统的抑制剂。为了进一步开发水杨酰腙类化合物，我们应用了骨架跃迁的方法来取代化合物的核心片段。新型 2-(2-氨基嘧啶)-2,2-二氟乙醇支架被确定为水杨酰腙核心结构的可能类似物。本文描述了 2-(2-氨基嘧啶)-2,2-二氟乙醇文库的合成。
