Synthesis of a novel inhibitor against MRSA and VRE: Preparation from zerumbone ring opening material showing histidine-kinase inhibition

Zerumbone ring-opening derivative 2 inhibited autophosphorylation of the essential histidine protein kinase (HPK), YycG, existing in Bacillus subtilis constituting a two-component system (TCS). However, it did not inhibit drug-resistant bacterium such as MRSA and VRE. Tryptophan derivative 34 also could be regulated by a TCS system like 2. In addition, 34 showed good inhibition against MRSA and VRE.

Graphical abstractThe synthesis of the novel YycG inhibitor 34 (IC50 = 43.9 μM) showing growth inhibition against MRSA and VRE is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide