Bacterial transferase MraY inhibitors: Synthesis and biological evaluation |
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| Authors: | Delphine Lecerclé Anthony Clouet Bayan Al-Dabbagh Muriel Crouvoisier Ahmed Bouhss Christine Gravier-Pelletier Yves Le Merrer |
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| Affiliation: | 1. Université Paris Descartes, UMR 8601 CNRS, Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, 45 rue des Saints-Pères, 75006 Paris, France;2. Université Paris-Sud, IBBMC, UMR 8619 CNRS, Enveloppes Bactériennes et Antibiotiques, Bât. 430, 91405 Orsay, France |
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| Abstract: | New inhibitors of the bacterial transferase MraY are described. Their structure is based on an aminoribosyl-O-uridine like scaffold, readily obtained in two key steps. The amino group can be coupled with proline or guanylated. Alternatively, these amino, prolinyl or guanidinyl groups can be introduced through a triazole linker. Biological evaluation of these compounds on MraY from Bacillus subtilis revealed interesting inhibitory activity for both amino compounds. |
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