Bottromycin derivatives: Efficient chemical modifications of the ester moiety and evaluation of anti-MRSA and anti-VRE activities

Novel bottromycin derivatives were synthesized from bottromycin A2 via a hydrazide derivative as a common intermediate. Seventeen derivatives were subjected to in vitro evaluation against drug-resistant gram-positive bacteria. Some compounds showed potent anti-MRSA and anti-VRE activity, as did bottromycin A2. Notably, a propyl ketone derivative exhibited good antibacterial activity with excellent metabolite stability.

Graphical abstractSeventeen novel bottromycin derivatives were synthesized via a key intermediate BTM hydrazide (3) to evaluate for their anti-MRSA and anti-VRE activities.Figure optionsDownload full-size imageDownload as PowerPoint slide