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.
