Novel pyridobenzimidazole derivatives exhibiting antifungal activity by the inhibition of β-1,6-glucan synthesis
详细信息 查看全文
- 作者：Hiroshi Takeshita ; Jun Watanabe ; Yoichi Kimura ; Katsuhiro Kawakami ; Hisashi Takahashi ; Makoto Takemura ; Akihiro Kitamura ; Kazuhiko Someya ; Ryohei Nakajima
- 关键词：Antifungal ; β ; -1 ; 6-Glucan ; Cell wall ; Pyridobenzimidazole ; Candida glabrata
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2010
- 出版时间：1 July 2010
- 年：2010
- 卷：20
- 期：13
- 页码：3893-3896
- 全文大小：312 K
文摘
Based on the HTS hit compound 1a, an inhibitor of β-1,6-glucan synthesis, we synthesized novel pyridobenzimidazole derivatives and evaluated their antifungal activity. Among the compounds synthesized, we identified the potent compound 15e, which exhibits excellent activity superior to fluconazole against both Candida glabrata and Candida krusei. From the SAR study, we revealed essential moieties for antifungal activity.