Metal-Mediated Inhibition of Escherichia c oli Methionine Aminopeptidase: Structure-Activity Relationships and Development of a Novel Scoring Function for Metal- …

R Schiffmann, A Neugebauer…

Index: Schiffmann, Rolf; Neugebauer, Alexander; Klein, Christian D. Journal of Medicinal Chemistry, 2006 , vol. 49, # 2 p. 511 - 522

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Citation Number: 68

Abstract

We report the discovery of thiabendazole as a potent inhibitor (K i= 0.4 μM) of Escherichia coli methionine aminopeptidase (ecMetAP) and the synthesis and pharmacological evaluation of thiabendazole congeners with activity in the upper nanomolar range. Elucidation of the X-ray structure of ecMetAP in complex with thiabendazole and an unrelated inhibitor that was independently described by another group showed that that ...