Design, Synthesis and in vitro Biochemical Activity of Novel Amino Acid Sulfonohydrazide Inhibitors of MurC

作者：Frlan Rok; Kovac Andreja; Blanot Didier; Gobec Stanislav; Pecar Slavko; Obreza Ales^*

来源：Acta Chimica Slovenica, 2011, 58(2): 295-310.

• MurC
• MurD
• inhibitors
• antibacterial
• sulfonohydrazide
• hydrazide

Mur ligases are essential enzymes involved in the cytoplasmic steps of peptidoglycan synthesis which remain attractive, yet unexploited targets. In order to develop new antibacterial agents, we have designed a series of new MurC and Mur-D inhibitors bearing amino acid sulfonohydrazide moiety. The L-Leu series of this class displayed the highest enzyme inhibition with IC50 in the concentration range between 100 and 500 mu M, with L-Thr, L-Pro and L-Ala derivatives being inactive. The most promising compound of the series also expressed weak antibacterial activity against S. aureus with MIC = 128 mu g/mL.

• 出版日期2011