Synthesis of novel 5-amino-thiazolo[4,5-d]pyrimidines as E. coli and S. aureus SecA inhibitors |
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| Authors: | Jang Mi-Yeon De Jonghe Steven Segers Kenneth Anné Jozef Herdewijn Piet |
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| Institution: | a Katholieke Universiteit Leuven, Rega Institute for Medical Research, Laboratory of Medicinal Chemistry, Minderbroedersstraat 10, 3000 Leuven, Belgium
b Katholieke Universiteit Leuven, Rega Institute for Medical Research, Laboratory of Bacteriology, Minderbroedersstraat 10, 3000 Leuven, Belgium |
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| Abstract: | An efficient synthesis of a library of 5-amino-thiazolo4,5-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. |
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| Keywords: | Thiazolo[4 5-d]pyrimidines SecA Bacterial preprotein secretion Inhibitor ATPase |
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