2092352-48-0
Chemical Structure
DS-2969b
- CAS No.: 2092352-48-0
- Formula:C17H25ClN6O3S
- Molecular Weight:428.94
IUPAC Name: 5-chloro-4-ethyl-N-((3S,4R)-1-(5-(2-hydroxypropan-2-yl)-1,3,4-thiadiazol-2-yl)-3-methoxypiperidin-4-yl)-1H-imidazole-2-carboxamide
InChIKey: RFKLYBAHWNXIDR-MNOVXSKESA-N
SMILES: O=C(C1=NC(CC)=C(Cl)N1)N[C@H]2[C@@H](OC)CN(C3=NN=C(C(C)(O)C)S3)CC2
Biological Activity: DS-2969b is an orally active GyrB inhibitor with antibacterial activity. DS-2969b is is active against Clostridium difficile infection (MIC90: 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[1][2].
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DS-2969b | DS-2969b is an orally active GyrB inhibitor with antibacterial activity. DS-2969b is is active against Clostridium difficile infection (MIC90: 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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References
- [1]. Mathur T, et al. In Vitro and In Vivo Activities of DS-2969b, a Novel GyrB Inhibitor, against Clostridium difficile. Antimicrob Agents Chemother. 2018 Mar 27;62(4):e02157-17. [Content Brief]
- [2]. Vandell AG, et al. Phase 1 Study To Assess the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Multiple Oral Doses of DS-2969b, a Novel GyrB Inhibitor, in Healthy Subjects. Antimicrob Agents Chemother. 2018 Apr 26;62(5):e02537-17. [Content Brief]
