Synthesis and activities of bactobolin derivatives having new functionality at C-3

Abstract

Some derivatives of bactobolin were prepared from bactobolin (1) by transformation of the dichloromethyl group at C-3 to the hydroxymethyl, carboxylic acid, methanesulfonyloxymethyl and aldehydeoxime groups. The derivatives proved to be less active than the parent antibiotic 1 against bacteria as well as cytotoxicity, indicating that the functionality at C-3 considerably influences the biological activity.