Combinatorial modification of natural products: synthesis and in vitro analysis of derivatives of thiazole peptide antibiotic GE2270 A: A-ring modifications
✍ Scribed by Jeffrey Clough; Shaoqing Chen; Eric M. Gordon; Corinne Hackbarth; Stuart Lam; Joaquim Trias; Richard J. White; Gianpaolo Candiani; Stefano Donadio; Gabriella Romanò; Romeo Ciabatti; Jeffrey W. Jacobs
- Book ID
- 104364105
- Publisher
- Elsevier Science
- Year
- 2003
- Tongue
- English
- Weight
- 228 KB
- Volume
- 13
- Category
- Article
- ISSN
- 0960-894X
No coin nor oath required. For personal study only.
✦ Synopsis
Thiazole peptide GE2270 A (1) possesses potent antimicrobial activity against many gram-positive pathogens, including methicillin resistant Staphylococcus aureus (S. aureus, MRSA; MIC 90 =0.06 mg/mL) and vancomycin resistant Enterococcus spp. (VRE; MIC 90 =0.03 mg/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.