Synthesis of 2-(2-Aminopyrimidine)-2,2-difluoroethanols as Potential Bioisosters of Salicylidene Acylhydrazides

被引：8

作者：

Dahlgren, Markus K. ^{[1
]}

Oberg, Christopher T. ^{[1
]}

Wallin, Erika A. ^{[1
]}

Janson, Par G. ^{[1
]}

Elofsson, Mikael ^{[1
]}

机构：

[1] Umea Univ, Dept Chem, SE-90187 Umea, Sweden

来源：

MOLECULES | 2010年 / 15卷 / 06期

关键词：

scaffold hopping; Reformatsky reaction; salicylidene acylhydrazide; type III secretion; SMALL-MOLECULE INHIBITORS; ENTERICA SEROVAR TYPHIMURIUM; III PROTEIN SECRETION; CHLAMYDIA-TRACHOMATIS; IDENTIFICATION; YERSINIA; CYCLE; VIRULENCE; BLOCK;

D O I：

10.3390/molecules15064423

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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-aminopyrimidine)-2,2-difluoroethanol scaffold was identified as a possible analog to the salicylidene acylhydrazide core structure. The synthesis of a library of 2-( 2- aminopyrimidine)-2,2- difluoro-ethanols is described in this paper.

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收藏

页码：4423 / 4438

页数：16

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