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

Abstract:

: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.

journal_name

Bioorg Med Chem

authors

Jang MY,De Jonghe S,Segers K,Anné J,Herdewijn P

doi

10.1016/j.bmc.2010.10.027

subject

Has Abstract

pub_date

2011-01-01 00:00:00

pages

702-14

issue

1

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(10)00950-8

journal_volume

19

pub_type

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