TenNor Discloses TNP-2198 for the Treatment of H. pylori Infections in the Journal of Medicinal Chemistry February 18, 2022
TNP-2198, a stable conjugate of a rifamycin pharmacophore and a nitroimidazole pharmacophore, has been designed, synthesized, and evaluated as a novel dual-targeted antibacterial agent for the treatment of microaerophilic and anaerobic bacterial infections. TNP-2198 exhibits greater activity than a 1:1 molar mixture of the parent drugs and exhibits activity against strains resistant to both rifamycins and nitroimidazoles. A crystal structure of TNP-2198 bound to a Mycobacterium tuberculosis RNA polymerase transcription initiation complex reveals that the rifamycin portion of TNP-2198 binds to the rifamycin binding site on RNAP and the nitroimidazole portion of TNP-2198 interacts directly with the DNA template-strand in the RNAP active-center cleft, forming a hydrogen bond with a base of the DNA template strand. TNP-2198 is currently in Phase 2 clinical development for the treatment of Helicobacter pylori infection, Clostridioides difficile infection, and bacterial vaginosis.
Link to the article: https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c02045
About TenNor Therapeutics
TenNor Therapeutics is a clinical-stage company specialized in the discovery and development of differentiated new drug products in diseases associated with bacterial infection and metabolism. TenNor possesses a unique multi-targeting drug conjugate technology platform and a strong new drug development pipeline with global IP protection. Several products are currently in late stage of clinical development, targeting H. pylori infection, implanted medical device infections, hepatic encephalopathy and irritable bowel syndrome with diarrhea. The company is committed to address the unmet needs in the disease area and provide safe and effective therapies for patients in China and around the world.
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