Discovery of a Novel Series of Semisynthetic Vancomycin Derivatives Effective against Vancomycin-Resistant Bacteria

详细信息    查看全文

• 作者：Yuki Nakama ; Osamu Yoshida ; Masanori Yoda ; Keisuke Araki ; Yuri Sawada ; Jun Nakamura ; Shu Xu ; Kenji Miura ; Hideki Maki ; Hirokazu Arimoto
• 刊名：Journal of Medicinal Chemistry
• 出版年：2010
• 出版时间：March 25, 2010
• 年：2010
• 卷：53
• 期：6
• 页码：2528-2533
• 全文大小：825K
• 年卷期：v.53,no.6(March 25, 2010)
• ISSN：1520-4804

文摘

Novel semisynthetic vancomycin derivatives with antibacterial activity against vancomycin-resistant S. aureus (VRSA) were prepared. Replacement of Cl groups of vancomycin by Suzuki−Miyaura cross-coupling reaction, which gave the title compounds, is described for the first time. Introduction of a carbon substituent at the amino acid residue 2 of vancomycin led to an enhancement of antibacterial activity against vancomycin-resistant strains, whereas the additional introduction at the amino acid residue 6 resulted in a reduction in activity even against vancomycin-susceptible strains.