Synthesis and antibacterial activity of nocathiacin I analogues

Bioorganic & Medicinal Chemistry Letters
B Narasimhulu NaiduYasutsugu Ueda

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.

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