Author/Authors :
Sulan Yao، نويسنده , , Paulo W.M. Sgarbi، نويسنده , , Kenneth A. Marby، نويسنده , , David Rabuka، نويسنده , , Sean M. OʹHare، نويسنده , , Mayling L. Cheng، نويسنده , , Mrunali Bairi، نويسنده , , Changyong Hu، نويسنده , , San-Bao Hwang، نويسنده , , Chan-Kou Hwang، نويسنده , , Yoshi Ichikawa، نويسنده , , Pamela Sears-Rogan، نويسنده , , Steven J. Sucheck، نويسنده ,
Abstract :
Glyco-optimization (OPopSTM) of aminoglycosides has been performed by replacing the existing sugar moiety with a variety of sugar derivatives. Glycosylation of the 6-position of nebramine provided a library of novel 4,6-linked aminoglycosides (AMGs). Among them, compounds 8b,g,i,l, and 8u with 2″-amino, 2″,3″-diamino, 2″,4″-diamino, 3″,4″-diamino, 3″-amino groups, respectively, showed significant antimicrobial activity against Gram-(+) and -(−) bacteria. Several were particularly potent against Pseudomonus aeruginosa with MICs in the 1–2 μg/mL range.
