Bis(indole) alkaloids as sortase A inhibitors from the sponge Spongosorites sp.

作者: Ki-Bong Oh , Woongchon Mar , Sanghee Kim , Ji-Yun Kim , Mi-Na Oh

DOI: 10.1016/J.BMCL.2005.08.021

关键词: Sortase AEnzyme inhibitorVirulenceSortaseIndole testAntibacterial agentStaphylococcus aureusBiochemistryEnzymeChemistryStereochemistryOrganic chemistryClinical biochemistryMolecular medicineMolecular biologyDrug discoveryPharmaceutical Science

摘要: A new bis(indole) alkaloid (9) of the hamacanthin class along with previously reported compounds related structural classes, topsentin (1-4) and (5-8), was isolated from marine sponge Spongosorites sp. their inhibitory activities toward sortase (SrtA) that play key roles in cell-wall protein anchoring virulence Staphylococcus aureus were evaluated. Our studies have identified a series SrtA inhibitors, providing basis for further development potent inhibitors. The preliminary structure-activity relationship, to elucidate essential requirements, has been described. fibronectin-binding activity data highlight potential these treatment S. infections via inhibition activity.

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