Discovery of Inhibitors of Burkholderia pseudomallei Methionine Aminopeptidase with Antibacterial Activity

作者：Wangtrakuldee Phumvadee; Byrd Matthew S; Campos Cristine G; Henderson Michael W; Zhang Zheng; Clare Michael; Masoudi Ali; Myler Peter J; Horn James R; Cotter Peggy A; Hagen Timothy J^*

来源：ACS Medicinal Chemistry Letters, 2013, 4(8): 699-703.

DOI：10.1021/ml400034m

• BpMetAP1
• methionine aminopeptidase inhibitor
• melioidosis
• Burkholderia pseudomallei

Evaluation of a series of MetAP inhibitors in an in vitro enzyme activity assay led to the first identification of potent molecules that show significant growth inhibition against Burkholderia pseudomallei. Nitroxoline analogues show excellent inhibition potency in the BpMetAP1 enzyme activity assay with the lowest IC50 of 30 nM and inhibit the growth of B. pseudomallei and B. thailandensis at concentrations >= 31 mu M.

• 出版日期2013-8