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更新于：2026-09-04

Rafoxanide

更新于：2026-09-04

概要

概要

基本信息

药物类型

小分子化药

别名

NSC-355278

靶点

OSR1 x STK39

作用方式

抑制剂

作用机制

OSR1 inhibitors(odd-skipped related transcription factor 1 inhibitors)、STK39抑制剂(serine/threonine kinase 39 inhibitors)

治疗领域

心血管疾病

在研适应症

高血压

非在研适应症-

原研机构

University of Birmingham

在研机构

University of Birmingham

非在研机构-

权益机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构/序列

分子式C19H11Cl2I2NO3

InChIKeyNEMNPWINWMHUMR-UHFFFAOYSA-N

CAS号22662-39-1

关联

100 项与 Rafoxanide 相关的临床结果

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100 项与 Rafoxanide 相关的转化医学

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100 项与 Rafoxanide 相关的专利（医药）

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220

项与 Rafoxanide 相关的文献（医药）

2026-05-05·Microbiology Spectrum

Synthesis and synergistic antibacterial activity of rafoxanide derivative as a novel drug for potentiating colistin activity

Article

作者: Zhai, Yajun ; Liu, Qiange ; Liu, Peiyi ; Li, Zibo ; Shao, Haotian ; Yang, Guoyu ; He, Dandan ; Ma, Xiaoyuan ; Hu, Gongzheng ; Wu, Hua

ABSTRACT:

Antimicrobial resistance poses a significant global public health challenge in the 21st century, with multidrug resistance in gram-negative bacteria being particularly severe. Colistin (COL) is considered the “last-resort” for treating such infections. Still, its efficacy is significantly reduced due to the emergence and prevalence of mobile colistin resistance (MCR)-mediated acquired drug resistance. Based on the synergistic antibacterial mechanism between the anthelmintic rafoxanide (RAF) and COL, we synthesized a novel RAF derivative (named as dikalisuan) through a carboxymethylation method, and its structure was confirmed using 1 H NMR, 13 C NMR, and HRMS. In vitro evaluation indicated that the derivatized product had no antibacterial activity (minimum inhibitory concentration [MIC] > 512 µg/mL). However, when used in combination with COL, it showed a significantly synergistic effect (fractional inhibitory concentration index [FICI] < 0.5) on mcr-1- positive and -negative resistant strains, including Escherichia coli , Salmonella , Klebsiella pneumoniae , and Acinetobacter baumannii . Notably, the synergistic bactericidal effect was optimal at a moderate concentration of 8 μg/mL. Furthermore, within the concentration range of 2 to 128 μg/mL, dikalisuan alone or in combination with COL (2 μg/mL) showed no significant hemolysis of red blood cells or cytotoxicity. This derivative provides a new strategy for developing adjuvants against multidrug-resistant bacteria and lays the foundation for the structural modification of anthelmintic salicylanilides.

IMPORTANCE:

Antimicrobial resistance in gram-negative bacteria is a critical global health threat, with colistin (COL) being a “last-resort” treatment. However, rising resistance has blunted its effectiveness. This study developed a new derivative of rafoxanide (RAF). While this new compound itself is not antibacterial, it effectively potentiates COL’s power against resistant bacteria when used in combination. This strategy offers a promising approach to extend the lifespan of our current antibiotics and provides a new weapon in the fight against difficult-to-treat drug-resistant bacteria.

2026-03-28·Zhong nan da xue xue bao. Yi xue ban = Journal of Central South University. Medical sciences

[Antibacterial activity and mechanism of the antiparasitic drug resorantel against Staphylococcus epidermidis].

Article

作者: Li, Yimin ; Lu, Lihua ; Wu, Yong ; Li, Mengna ; Xiao, Dan ; Huang, Guanqing ; Guo, Shaowei

OBJECTIVES:

Staphylococcus epidermidis (S. epidermidis) is a common opportunistic pathogen in clinical settings. The widespread misuse of antibiotics has led to a continuous increase in its antimicrobial resistance, greatly complicating treatment. Drug repurposing, characterized by low cost, high safety, and short development cycles, represents an effective strategy for combating drug-resistant bacterial infections. This study aims to investigate the antibacterial activity of the antiparasitic drug resorantel against S. epidermidis and to preliminarily elucidate its antibacterial mechanism.

METHODS:

The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of resorantel against S. epidermidis were determined using the broth microdilution method. Disk diffusion assays, 2, 3-Bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilid (XTT) assays, and time‑kill curves were employed to evaluate the susceptibility of S. epidermidis to resorantel. Serial induction experiments were conducted to assess the potential for resistance development. Crystal violet staining and XTT assays were used to evaluate the inhibitory and eradication effects of resorantel on biofilms. The checkerboard microdilution method was performed to investigate the combined effects of rafoxanide with conventional antibiotics. Antibacterial mechanisms were preliminarily explored by assessing membrane permeability, proton motive force, intracellular adenosine triphosphate (ATP) levels, and propidium iodide staining. Finally, a murine skin abscess model was established to evaluate the in vivo antibacterial activity of resorantel.

RESULTS:

The MIC and MBC of resorantel against S. epidermidis were 2 μg/mL and 16 μg/mL, respectively. Disk diffusion assays demonstrated a pronounced antibacterial effect of resorantel against S. epidermidis. XTT assay results demonstrated that resorantel significantly reduced the viability of S. epidermidis (P<0.05). Time‑kill curve analysis indicated that even 1/4×MIC of resorantel effectively inhibited bacterial proliferation. After continuous exposure for 15 d, S. epidermidis did not develop resistance to resorantel. Crystal violet staining and XTT staining both revealed that 1 μg/mL resorantel significantly inhibited biofilm formation, while 2 μg/mL resorantel significantly reduced preformed biofilms (all P<0.05). Resorantel altered the proton motive force, inhibited intracellular ATP synthesis, and disrupted bacterial cell membrane integrity. In the murine skin abscess model, resorantel treatment significantly reduced the bacterial burden within abscess tissues (all P<0.05).

CONCLUSIONS:

Resorantel exhibits both in vitro and in vivo antibacterial activity against S. epidermidis. Its antibacterial mechanism involves disruption of bacterial membrane integrity and proton motive force, as well as inhibition of intracellular ATP synthesis.

2025-11-01·JOURNAL OF VETERINARY PHARMACOLOGY AND THERAPEUTICS

Albendazole and Clorsulon in Fasciola hepatica Control: Integrated Pharmacokinetic and Flukicidal Eficacy Assessment in Sheep

Article

作者: Ceballos, L. ; Pruzzo, C. ; Alvarez, L. ; Chiappetta, V. ; Cantón, C. ; Lanusse, C.

ABSTRACT:

Fasciola hepatica causes fasciolosis, a growing zoonotic disease that affects both livestock and humans worldwide. The main strategy to control fasciolosis in livestock animals, is based on drugs such as triclabendazole (TCBZ), albendazole (ABZ), clorsulon (CLOR), nitroxynil, closantel, and rafoxanide. Only TCBZ is available for F. hepatica control in human medicine and its resistance is growing. The use of drug combinations has been proposed as a strategy to delay it. This study compares the pharmacokinetics and flukicidal efficacy of ABZ + CLOR when administered together or separately in sheep infected with F. hepatica . Enhanced systemic exposure of the ABZ sulphoxide metabolite was observed after the co‐administration ABZ + CLOR compared to the ABZ alone treatment. The CLOR disposition kinetics was not affected by its co‐administration with ABZ. The flukicidal clinical efficacy was 85% (ABZ), 92% (CLOR) and 100% (ABZ + CLOR), respectively. The work described here contributes to the characterization of the disposition kinetics of both flukicidal molecules showing that the combined ABZ and CLOR therapy may enhance the efficacy against F. hepatica in sheep.

100 项与 Rafoxanide 相关的药物交易

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