2‐Nitrobenzyl Esters of Penam and Cephem Derivatives as Inhibitors of Penicillin‐Binding Proteins
作者： Cédric Brulé , Jérôme Grugier , Alain Brans , Bernard Joris , Eric Sauvage
关键词:
摘要: Nitroveratrole esters (i.e. 4,5-dimethoxy-2-nitrobenzyl (NV) esters) of penicillin and cephalosporin derivatives have been prepared in the course a program dedicated to photosensitive protein microarrays. Surprisingly, some molecules revealed be acylating inhibitors R39 BlaR-CTD proteins (two representative Penicillin Binding Proteins (PBPs)), while being bad substrates beta-lactamases (bacterial defense enzymes). Electrostatic potential maps docking experiments showed that 2-nitro group NV could play role carboxylate penam series.
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