Sunazuka Toshiaki, Shudo Hiroko, Nagai Kenichiro, Yoshida Kiminari, Yamaguchi Yukie, Hanaki Hideaki, Omura Satoshi
Kitasato Institute for Life Sciences and Graduate School of Infection Control Sciences, Kitasato University and The Kitasato Institute, Minato-ku, Tokyo, Japan.
J Antibiot (Tokyo). 2008 Mar;61(3):175-84. doi: 10.1038/ja.2008.127.
18-amino-4''-O-benzoyl-4'''-N-demethyl-18-deoxospiramycins were designed and synthesized. Synthetic strategy involved selective demethylation of the dimethylamino group in forosamine, benzoylation of the hydroxyl group at the C4'' position and reductive N-amination of the formyl group. Antibacterial characteristics of spiramycin derivatives were tested. The derivatives exhibited promising activity against drug-resistant bacterial strains.
设计并合成了18-氨基-4''-O-苯甲酰基-4'''-N-去甲基-18-脱氧螺旋霉素。合成策略包括福洛糖胺中二甲氨基的选择性脱甲基、C4''位羟基的苯甲酰化以及甲酰基的还原N-胺化。测试了螺旋霉素衍生物的抗菌特性。这些衍生物对耐药菌株表现出有前景的活性。
