Tetracyclic indolines as a novel class of β-lactam-selective resistance-modifying agent for MRSA

详细信息    查看全文

• 作者：Yugen Zhu¹ ; Lakota Cleaver¹ ; Wei Wang ; Jessica D. Podoll ; Shane Walls ; Austin Jolly ; Xiang Wang ; ^{xiang.wang@colorado.edu}
• 关键词：β-lactam ; Antibiotic resistance ; Methicillin-resistant Staphylococcus aureus ; Resistance-modifying agent ; Structure-activity relationship ; Indoline alkaloids
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：130-142
• 全文大小：727 K
• 卷排序：125

文摘

A novel class of tetracyclic indolines was discovered in a β-lactam potentiator screen in MRSA. The compound selectively potentiates β-lactams but not any other classes of antibiotics. This novel class of compounds does not have antibacterial activity on its own, nor directly inhibit the β-lactamase activity. Structure-activity relationship (SAR) study identified a more potent analogue with reduced mammalian cell toxicity.