Bacterial transferase MraY inhibitors: Synthesis and biological evaluation

…, M Crouvoisier, A Bouhss, C Gravier-Pelletier…

Index: Lecercle, Delphine; Clouet, Anthony; Al-Dabbagh, Bayan; Crouvoisier, Muriel; Bouhss, Ahmed; Gravier-Pelletier, Christine; Le Merrer, Yves Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 12 p. 4560 - 4569

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Citation Number: 18

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 ...