Synthesis and antibacterial activity of nocathiacin I analogues.

Abstract 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.