摘要
利福霉素因其熟练的绝育能力而被认为是结核病(TB)治疗的里程碑。目前,现有的结核病治疗很复杂,需要很长的持续时间,这最终导致患者依从性失败。一些新的利福霉素衍生物,即利法美坦、TNP-2092(利福霉素-喹啉-喹啉杂交种)和 TNP-2198(利福霉素-硝基咪唑杂交种)正在进行临床试验,这些试验试图克服与结核病治疗相关的问题。所进行的评价旨在比较这些利福霉素的药代动力学、药效学和安全性,包括利福拉齐(II期试验中终止的另一种衍生物)和已批准的利福霉素。微生物的耐药性是与抗生素相关的必要考虑因素。简要描述了微生物菌株对利福霉素的耐药性发展潜力和化学概述,以及利福霉素的构效关系(SAR)。此外,还讨论了与利福霉素相关的问题。我们预计,在不久的将来,新出现的利福霉素将成为结核病治疗的潜在工具。
关键词: 利福霉素,利福美坦,利福拉齐,TNP-2092,TNP-2198,安沙霉素。
Current Medicinal Chemistry
Title:A Comparative Insight on the Newly Emerging Rifamycins: Rifametane, Rifalazil, TNP-2092 and TNP-2198
Volume: 29 Issue: 16
关键词: 利福霉素,利福美坦,利福拉齐,TNP-2092,TNP-2198,安沙霉素。
摘要: 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.
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Cite this article as:
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
DOI https://dx.doi.org/10.2174/0929867328666210806114949 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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