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 A 、 Enzyme inhibitor 、 Virulence 、 Sortase 、 Indole test 、 Antibacterial agent 、 Staphylococcus aureus 、 Biochemistry 、 Enzyme 、 Chemistry 、 Stereochemistry 、 Organic chemistry 、 Clinical biochemistry 、 Molecular medicine 、 Molecular biology 、 Drug discovery 、 Pharmaceutical 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.