Combinatorial modification of natural products: synthesis and in vitro analysis of derivatives of thiazole peptide antibiotic GE2270 A: A-ring modifications |
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Authors: | Clough Jeffrey Chen Shaoqing Gordon Eric M Hackbarth Corinne Lam Stuart Trias Joaquim White Richard J Candiani Gianpaolo Donadio Stefano Romanò Gabriella Ciabatti Romeo Jacobs Jeffrey W |
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Affiliation: | Vicuron, Inc., 34790 Ardentech Court, Fremont, CA 94555, USA. |
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Abstract: | 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 microg/mL) and vancomycin resistant Enterococcus spp. (VRE; MIC(90)=0.03 microg/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. |
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