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

Jang MY; De Jonghe S; Segers KAnne JHerdewijn P

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

机译：Synthesis of novel 5-amino-thiazolo(4,5-d)pyrimidines as E. coli and S. aureus SecA inhibitors.

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摘要

An efficient synthesis of a library of 5-amino-thiazolo4,5-dpyrimidines 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.

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《Bioorganic and medicinal chemistry》 |2011年第1期|702-714|共13页
作者
Jang MY; De Jonghe S; Segers KAnne JHerdewijn P;
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作者单位

Katholieke Universiteit Leuven, Rega Institute for Medical Research, Laboratory of Medicinal Chemistry, Minderbroedersstraat 10, 3000 Leuven, Belgium.;

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正文语种英语
中图分类药学;
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Synthesis of novel 5-amino-thiazolo(4,5-d)pyrimidines as E. coli and S. aureus SecA inhibitors.

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