Author/Authors :
Jeffrey Clough، نويسنده , , Shaoqing Chen، نويسنده , , Eric M. Gordon، نويسنده , , Corinne Hackbarth، نويسنده , , Stuart Lam، نويسنده , , Joaquim Trias، نويسنده , , Richard J. White، نويسنده , , Gianpaolo Candiani، نويسنده , , Stefano Donadio، نويسنده , , Gabriella Roman?، نويسنده , , Romeo Ciabatti، نويسنده , , Jeffrey W. Jacobs، نويسنده ,
Abstract :
Thiazole peptide GE2270 A (1) possesses potent antimicrobial activity against many gram-positive pathogens, including methicillin resistant Staphylococcus aureus (S. aureus, MRSA; MIC90=0.06 μg/mL) and vancomycin resistant Enterococcus spp. (VRE; MIC90=0.03 μg/mL); however its poor aqueous solubility has prohibited its development for the clinical treatment of infections. An integrated combinatorial and medicinal chemistry program was employed to identify derivatives of1 that retain activity but possess greatly enhanced aqueous solubility.
