Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 14, Pages 4575-4578Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.05.110
Keywords
Macrolide antibiotics; Desosamine; Erm resistance; Deoxygenation
Categories
Funding
- Direct For Mathematical & Physical Scien
- Division Of Chemistry [1150768] Funding Source: National Science Foundation
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Structural factors behind erm macrolide resistance were studied through synthesis of new macrolide derivates possessing truncated desosamine sugar moieties and subsequent determination of their antibacterial activity. Synthesized compounds with 2'-deoxy and 3'-desmethyl desosamine rings demonstrated decreased antibacterial activity on the native Staphylococcus aureus strain and were inactive against constitutively resistance S. aureus. The obtained results indicate that steric repulsion between the dimethylated A2058 and desosamine ring cannot be considered as a primary reason for erm-resistance. (C) 2012 Published by Elsevier Ltd.
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