TY - JOUR
T1 - 6″-thioether tobramycin analogues
T2 - Towards selective targeting of bacterial membranes
AU - Herzog, Ido M.
AU - Green, Keith D.
AU - Berkov-Zrihen, Yifat
AU - Feldman, Mark
AU - Vidavski, Roee R.
AU - Eldar-Boock, Anat
AU - Satchi-Fainaro, Ronit
AU - Eldar, Avigdor
AU - Garneau-Tsodikova, Sylvie
AU - Fridman, Micha
PY - 2012/6/4
Y1 - 2012/6/4
N2 - Amphiphilic tobramycin analogues with potent antibacterial activity against tobramycin-resistant bacteria were synthesized. Most analogues were found to be less prone to deactivation by aminoglycoside-modifying enzymes than tobramycin. These compounds target the bacterial membrane rather than the ribosome (see picture). The lipophilic residue of these analogues is key to their antibacterial potency and selectivity towards bacterial membranes.
AB - Amphiphilic tobramycin analogues with potent antibacterial activity against tobramycin-resistant bacteria were synthesized. Most analogues were found to be less prone to deactivation by aminoglycoside-modifying enzymes than tobramycin. These compounds target the bacterial membrane rather than the ribosome (see picture). The lipophilic residue of these analogues is key to their antibacterial potency and selectivity towards bacterial membranes.
KW - aminoglycoside-modifying enzymes
KW - amphiphiles
KW - antibiotics
KW - glycosides
KW - hemolysis
UR - https://www.scopus.com/pages/publications/84861636746
UR - https://www.scopus.com/pages/publications/84861636746#tab=citedBy
U2 - 10.1002/anie.201200761
DO - 10.1002/anie.201200761
M3 - Article
C2 - 22499286
AN - SCOPUS:84861636746
SN - 1433-7851
VL - 51
SP - 5652
EP - 5656
JO - Angewandte Chemie - International Edition
JF - Angewandte Chemie - International Edition
IS - 23
ER -