期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 19, 页码 5757-5762出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.07.139
关键词
MurA; Peptidoglycan; Tulipalines; Tuliposides
资金
- Deutsche Forschungsgemeinschaft [KL 1356]
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. (C) 2010 Elsevier Ltd. All rights reserved.
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