Compound ID | 2356

Vancomycin GR-MoTr conjugate

Synonym(s): V-r8

Class: Glycopeptide

Spectrum of activity: Gram-positive
Details of activity: Active against methicillin-resistant Staphylococcus aureus (planktonic and biofilm) and vancomycin-resistant Enterococci; targets lipid II and disrupts integrity of cytoplasmic membrane
Description: Semi-synthetic compound; vancomycin attached to D-octaarginine (r8) - a cell-penetrating guanidinium-rich molecular transporter (GR-MoTr); shows antibiofilm activity with MBEC 9.5-20 uM vs MRSA; minimal haemolytic activity (HC50 >320 uM), 50% cytotoxicity towards HaCaT cells observed at 10x MIC; reduced biofilm bacterial load in murine wound model
Institute where first reported: Department of Chemical and Systems Biology, Stanford University, Stanford, California 94305, United States
Year first mentioned: 2018
Development status: Experimental

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