期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 15, 期 22, 页码 4927-4931出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.08.021
关键词
bis(indole) alkaloids; sponge; sortase A inhibitory activity
A new bis(indole) alkaloid (9) of the hamacanthin class along with the previously reported compounds of the related structural classes, topsentin class (1-4) and hamacanthin class (5-8), was isolated from the marine sponge Spongosorites sp. and their inhibitory activities toward sortase A (SrtA) that play key roles in cell-wall protein anchoring and virulence in Staphylococcus aureus were evaluated. Our studies have identified a series of SrtA inhibitors, providing the basis for further development of potent inhibitors. The preliminary structure-activity relationship, to elucidate the essential structural requirements, has been described. The fibronectin-binding activity data highlight the potential of these compounds for the treatment of S. aureus infections via inhibition of SrtA activity. (c) 2005 Elsevier Ltd. All rights reserved.
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