Synthesis of novel 5-amino-thiazolo [4, 5-d] pyrimidines as E. coli and S. aureus SecA inhibitors

…, S De Jonghe, K Segers, J Anné, P Herdewijn

文献索引：Jang, Mi-Yeon; Jonghe, Steven De; Segers, Kenneth; Anne, Jozef; Herdewijn, Piet Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 1 p. 702 - 714

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被引用次数: 38

摘要

An efficient synthesis of a library of 5-amino-thiazolo [4, 5-d] pyrimidines is reported. Regioselective displacements of chlorines, as well as regioselective diazotation reactions are described, which allow the introduction of structural diversity on the scaffold by consecutive reactions. Screening of this focused library led to the discovery of SecA inhibitors from Escherichia coli and Staphylococcus aureus.