Bioorganic & Medicinal Chemistry Letters 2010-10-01

Structure-activity relationships of tulipalines, tuliposides, and related compounds as inhibitors of MurA.

Thomas Mendgen, Therese Scholz, Christian D Klein

文献索引:Bioorg. Med. Chem. Lett. 20 , 5757-62, (2010)

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摘要

The enzyme MurA performs an essential step in peptidoglycan biosynthesis and is therefore a target for the discovery of novel antibacterial compounds. We report here the inhibition of MurA by natural products from tulips (tulipalines and tuliposides), and the structure-activity relationships of various derivatives. The inhibition of MurA can be related to antibacterial activity, and MurA is probably one of the relevant molecular targets of the tulipaline derivatives. MurA inhibition by this class of compounds depends on the presence of the substrate UNAG, which indicates non-covalent suicide inhibition as observed previously for cnicin. With respect to selectivity, however, the reactivity against arbitrary sulfhydryl groups, such as in glutathione, could not yet be sufficiently separated from MurA inhibition in the present dataset.Copyright (c) 2010 Elsevier Ltd. All rights reserved.


相关化合物

  • 丙酮缩甘油
  • α-亚甲基-γ-丁内酯
  • 2-溴甲基丙烯酸甲酯

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