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[1][2].

Product Specifications

CAS Number

[2092352-48-0]

UNSPSC

12352005

Target

Bacterial; DNA/RNA Synthesis

Related Pathways

Anti-infection; Cell Cycle/DNA Damage

Field of Research

Infection

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

Molecular Formula

C17H25ClN6O3S

Molecular Weight

428.94

References & Citations

[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. |[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.