Site-selective functionalization of glycopeptide antibiotics
AssigneeYale University
InventorsTejaskumar P. Pathak, Scott J. Miller
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AssigneeYale University
InventorsTejaskumar P. Pathak, Scott J. Miller
Estimating the term…
Site-selective functionalized glycopeptide antibiotics, methods of making and using are described herein. The compounds exhibit improved activity against methicillin-susceptible S. aureus (MSSA), methicillin-resistant S. aureus (MRSA), vancomycin-sensitive S. aureus (VSE), vancomycin-resistant enterococci (VRE), or combinations thereof. The compounds can be administered as the neutral free acid or free base or can be administered as a pharmaceutically acceptable acid-addition or base-addition salt. The compounds can be formulated with one or more pharmaceutically acceptable excipients to prepare pharmaceutical compositions. The compounds can be administered by a variety of routes of administration including enteral, parenteral, topical, or transmucosal.
A compound of Formula II:
The compound of 10, wherein R is selected from the group consisting of 4-decenoyl (A2-1), 9-methylnonanoyl (A2-2), decanoyl (A2-3), 8-methyldecanoyl (A2-4), 9-methyldecanoyl (A2-5).
Dependencies are inferred from the claim text.