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  • Title: Novel pyridobenzimidazole derivatives exhibiting antifungal activity by the inhibition of beta-1,6-glucan synthesis.
    Author: Takeshita H, Watanabe J, Kimura Y, Kawakami K, Takahashi H, Takemura M, Kitamura A, Someya K, Nakajima R.
    Journal: Bioorg Med Chem Lett; 2010 Jul 01; 20(13):3893-6. PubMed ID: 20605446.
    Abstract:
    Based on the HTS hit compound 1a, an inhibitor of beta-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.
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