Abstract

Alalevonadifloxacin (ALA, formerly described as WCK 2349) is a novel antibacterial drug developed to treat infections caused by Gram-positive bacteria. The current study was aimed to identify and quantify impurities in ALA. Mass spectrometry (MS) compatible reverse phase liquid chromatographic method was developed to identify the impurities in ALA. Three impurities were identified based on the molecular ion peak and their product ions. These impurities were synthesized and characterized using MS and nuclear magnetic resonance spectrometry. However, this method was unable to resolve the diastereomeric impurity, which is likely to be formed during synthesis. Therefore, another method was developed using YMC Chiral NEA-[S] as a chiral stationary phase and validated for quantification of all impurities including diastereomeric impurity. The developed method was employed for quality control and stability studies of the ALA drug substance used in pre-clinical and clinical studies.

中文翻译：

---

新型抗MRSA抗菌药物的杂质分析：Alalevonadifloxacin。

摘要

Alalevonadifloxacin（ALA，以前称为WCK 2349）是开发用于治疗革兰氏阳性细菌感染的新型抗菌药物。当前的研究旨在鉴定和定量ALA中的杂质。建立了质谱（MS）兼容的反相液相色谱方法，以鉴定ALA中的杂质。根据分子离子峰及其产物离子鉴定出三种杂质。使用MS和核磁共振波谱仪合成并表征了这些杂质。但是，该方法不能解决可能在合成过程中形成的非对映异构杂质。因此，开发了另一种使用YMC手性NEA- [S]作为手性固定相的方法，该方法经过验证可用于定量分析所有杂质，包括非对映异构体杂质。