Synthesis and antibacterial activity of nocathiacin I analogues

Stereoselective reduction of dehydroalanine double bond in nocathiacin I afforded the primary amide 2. Enzymatic hydrolysis of the amide 2 provided the carboxylic acid 3, which upon coupling with a variety of amines furnished amides 4–32. Some of these semi-synthetic derivatives have retained very good antibacterial activity and have improved aqueous solubility.

The synthesis and antibacterial activity of nocathiacin I analogues is described.Figure optionsDownload as PowerPoint slide