Author(s): Jakopovi IP, Krajai MB, Skugor MM, Stimac V, Pei D,
Abstract Share this page
Abstract Novel modifications of the desosamine sugar of 14- and 15-membered antibacterial macrolides, in which the desosamine was fused with N-substituted-1,3-oxazolidin-2-ones, were developed in order to completely suppress antibacterial activity and make them promising agents for other biological targets. The synthesis of such bicyclic desosamine derivatives, especially 1,3-oxazolidin-2-one formation, was optimized and conducted under mild conditions without a need for protection/deprotection steps for other functional groups. A focused series of novel desosamine-modified macrolide derivatives was prepared and their antibacterial activities tested. It was shown that these macrolide derivatives do not possess any residual antibacterial activity. Copyright © 2012 Elsevier Ltd. All rights reserved.
This article was published in Bioorg Med Chem Lett
and referenced in Journal of Environmental Analytical Chemistry