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Synthesis and activities of bactobolin derivatives having new functionality at C-3
Hayamitsu Adachi1, Yoshio Nishimura, Tomio Takeuchi
1Institute of Microbial Chemistry, Tokyo, Japan.
The Journal of Antibiotics
|March 29, 2002
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.