Adachi Hayamitsu, Nishimura Yoshio, Takeuchi Tomio
Institute of Microbial Chemistry, Tokyo, Japan.
J Antibiot (Tokyo). 2002 Jan;55(1):92-8. doi: 10.7164/antibiotics.55.92.
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.
通过将杆菌肽（1）中C-3位的二氯甲基转化为羟甲基、羧酸、甲磺酰氧基甲基和醛肟基，制备了一些杆菌肽衍生物。结果证明，这些衍生物在抗细菌活性以及细胞毒性方面均低于母体抗生素1，这表明C-3位的官能团对生物活性有显著影响。
