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

Kitayama T, Iwabuchi R, Minagawa S, Sawada S, Okumura R, Hoshino K, Cappiello J, Utsumi R

Department of Advanced Bioscience, Graduate School of Agriculture, Kinki University, Nara 631-8505, Japan. kitayama@nara.kindai.ac.jp

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.

Published 5 February 2007 in Bioorg Med Chem Lett, 17(4): 1098-101.
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