DS-2969b is an orally active GyrB inhibitor with antibacterial activity. DS-2969b is is active against Clostridium difficile infection (MIC 90 : 0.06 μg/mL), which is 2-, 16-, and 32-fold lower than those of Fidaxomicin ( HY-17580 ), Metronidazole ( HY-B0318 ), and Vancomycin ( HY-B0671 ), respectively. DS-2969b inhibits the supercoiling activity of C. difficile DNA gyrase. DS-2969b also exhibits activity against other Gram-positive anaerobes, including strict and facultative anaerobes. DS-2969b is safe and well tolerated in preclinical toxicology studies.
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