Synthesis and antibacterial activity of desosamine-modified macrolide derivatives |
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Authors: | LeTourneau Nicolas Vimal Pavan Klepacki Dorota Mankin Alexander Melman Artem |
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Institution: | Department of Chemistry & Biomolecular Science, Clarkson University, 8 Clarkson Ave., Potsdam, NY 13699-5810, United States. |
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Abstract: | 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. |
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