Abstract: 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.

Abstract: 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.