A Comparative Insight on the Newly Emerging Rifamycins: Rifametane, Rifalazil, TNP-2092 and TNP-2198

Title:A Comparative Insight on the Newly Emerging Rifamycins: Rifametane, Rifalazil, TNP-2092 and TNP-2198

Volume: 29 Issue: 16

Author(s): Adila Nazli, David L. He, Huacheng Xu, Zhi-Peng Wang*Yun He*

Affiliation:

• Chongqing Key Laboratory of Natural Product Synthesis and Drug Research, School of Pharmaceutical Sciences, Chongqing University, Chongqing 401331, P.R. China
• Chongqing Institute of Green and Intelligent Technology, Chinese Academy of Sciences, Chongqing, P.R. China
• Chongqing School, University of Chinese Academy of Sciences, Chongqing, P.R. China

• Chongqing Key Laboratory of Natural Product Synthesis and Drug Research, School of Pharmaceutical Sciences, Chongqing University, Chongqing 401331, P.R. China

Keywords: Rifamycins, rifametane, rifalazil, TNP-2092, TNP-2198, ansamycins.

Abstract: Rifamycins are considered a milestone for tuberculosis (TB) treatment because of their proficient sterilizing ability. Currently, available TB treatments are complicated and need a long duration, which ultimately leads to failure of patient compliance. Some new rifamycin derivatives, i.e., rifametane, TNP-2092 (rifamycin-quinolizinonehybrid), and TNP-2198 (rifamycin-nitromidazole hybrid) are under clinical trials, which are attempting to overcome the problems associated with TB treatment. The undertaken review is intended to compare the pharmacokinetics, pharmacodynamics and safety profiles of these rifamycins, including rifalazil, another derivative terminated in phase II trials, and already approved rifamycins. The emerging resistance of microbes is an imperative consideration associated with antibiotics. Resistance development potential of microbial strains against rifamycins and an overview of chemistry, as well as structure-activity relationship (SAR) of rifamycins, are briefly described. Moreover, issues associated with rifamycins are discussed as well. We expect that newly emerging rifamycins shall appear as potential tools for TB treatment in the near future.

Cite this article as:

Nazli Adila , He L. David, Xu Huacheng , Wang Zhi-Peng *, He Yun *, A Comparative Insight on the Newly Emerging Rifamycins: Rifametane, Rifalazil, TNP-2092 and TNP-2198, Current Medicinal Chemistry 2022; 29 (16) . https://dx.doi.org/10.2174/0929867328666210806114949