Pyrazolidine-3, 5-diones and 5-hydroxy-1 H-pyrazol-3 (2 H)-ones, inhibitors of UDP-N-acetylenolpyruvyl glucosamine reductase

…, J Shumsky, Y Yang, A Severin, G Singh…

Index: Gilbert, Adam M.; Failli, Amedeo; Shumsky, Jay; Yang, Youjun; Severin, Anatoly; Singh, Guy; Hu, William; Keeney, David; Petersen, Peter J.; Katz, Alan H. Journal of Medicinal Chemistry, 2006 , vol. 49, # 20 p. 6027 - 6036

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Citation Number: 62

Abstract

A series of pyrazolidine-3, 5-dione and 5-hydroxy-1 H-pyrazol-3 (2 H)-one inhibitors of Escherichia coli UDP-N-acetylenolpyruvyl glucosamine reductase (MurB) has been prepared. The 5-hydroxy-1 H-pyrazol-3 (2 H)-ones show low micromolar IC50 values versus E. coli MurB and submicromolar minimal inhibitory concentrations (MIC) against Staphylococcus aureus GC 1131, Enterococcus faecalis GC 2242, Streptococcus ...