628707-74-4Relevant academic research and scientific papers
Combinatorial modification of natural products: Synthesis and in vitro analysis of derivatives of thiazole peptide antibiotic GE2270 A: A-ring modifications
Clough, Jeffrey,Chen, Shaoqing,Gordon, Eric M.,Hackbarth, Corinne,Lam, Stuart,Trias, Joaquim,White, Richard J.,Candiani, Gianpaolo,Donadio, Stefano,Romano, Gabriella,Ciabatti, Romeo,Jacobs, Jeffrey W.
, p. 3409 - 3414 (2003)
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 of 1 that retain activity but possess greatly enhanced aqueous solubility.
