Structure–Activity Relationship Studies of the Tricyclic Indoline Resistance-Modifying Agent

نویسندگان

  • Le Chang
  • Jessica D. Podoll
  • Wei Wang
  • Shane Walls
  • Courtney P. O’Rourke
  • Xiang Wang
چکیده

Previously we discovered a tricyclic indoline, N-[2-(6-bromo-4-methylidene-2,3,4,4a,9,9a-hexahydro-1H-carbazol-4a-yl)ethyl]-4-chlorobenzene-1-sulfonamide (1, Of1), from bioinspired synthesis of a highly diverse polycyclic indoline alkaloid library, that selectively resensitizes methicillin-resistant Staphylococcus aureus strains to β-lactam antibiotics. Herein, we report a thorough structure-activity relationship investigation of 1, which identified regions of 1 that tolerate modifications without compromising activity and afforded the discovery of a more potent analogue with reduced mammalian toxicity.

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عنوان ژورنال:

دوره 57  شماره 

صفحات  -

تاریخ انتشار 2014