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Synthesis and biological evaluation of salicylate-based compounds as a novel class of methionine aminopeptidase inhibitors
Authors:Wang Wen-Long  Chai Sergio C  Ye Qi-Zhuang
Affiliation:Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, IN 46202, USA.
Abstract:A series of salicylate-based compounds were designed and synthesized based on the simple function group replacement from our previously reported catechol-containing inhibitors of methionine aminopeptidase (MetAP). Some of these salicylate derivatives showed similar potency and metalloform selectivity, and some showed considerable antibacterial activity. These findings are consistent with our previous conclusion that Fe(II) is the likely metal used by MetAP in bacterial cells and provide new lead structures that can be further developed as novel antibacterial agents.
Keywords:Salicylic acid   Metalloenzyme   Inhibition   Antibacterial   Drug discovery
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