Synonyms: CBR-2092 | TNP-2092
Compound class:
Synthetic organic
Comment: Rifaquizinone (formerly CBR-2092, then TNP-2092) is a rifamycin-quinolone hybrid antibacterial compound [2]. It exerts combined effects on bacterial RNA polymerase, DNA gyrase and DNA topoisomerase IV, although RNA polymerase has been reporetd as the primary cellular target [4]. Rifaquizinone was developed for potential to treat biofilm associated infections such as those caused by staphylococci [3-4]. Initial development was by Cumbre Pharmaceuticals, but it is now being taken forward by TenNor Therapeutics, hence the change in research code.
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References |
1. Fisher CR, Schmidt-Malan SM, Ma Z, Yuan Y, He S, Patel R. (2020)
In vitro activity of TNP-2092 against periprosthetic joint infection-associated staphylococci. Diagn Microbiol Infect Dis, 97 (3): 115040. [PMID:32354459] |
2. Ma Z, Lynch AS. (2016)
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections. J Med Chem, 59 (14): 6645-57. [PMID:27336583] |
3. Robertson GT, Bonventre EJ, Doyle TB, Du Q, Duncan L, Morris TW, Roche ED, Yan D, Lynch AS. (2008)
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: microbiology profiling studies with staphylococci and streptococci. Antimicrob Agents Chemother, 52 (7): 2324-34. [PMID:18443106] |
4. Robertson GT, Bonventre EJ, Doyle TB, Du Q, Duncan L, Morris TW, Roche ED, Yan D, Lynch AS. (2008)
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus. Antimicrob Agents Chemother, 52 (7): 2313-23. [PMID:18443108] |