engleski

Impurity profiling of azithromycin conjugates by LC- SPE/CRYO NMR methodology

Azithromycin belongs to an azalide subclass of 15- membered macrolide antibiotics. It was synthesized in the early 1980s as a semi- synthetic derivative of erythromycin.[1] With a much improved pharmacokinetic properties over erythromycin, azithromycin became the most widely used broad- spectrum antibiotic.[2] Thiosemicarbazones belong to a large group of thiourea derivatives and are well known as antibacterial, antiviral, anti- inflammatory, antifungal and anticancer therapeutics.[3] Furthermore, a new multi- functional thiosemicarbazones were designed to treat Alzheimer and malaria.[4, 5] Conjugation of the azithromycin and thiosemicarbazone derivatives resulted in novel compounds which showed good activity against some Gram positive and Gram negative bacterial strains. Modern approach to the drug impurity profiling is based on the use of hyphenated systems, such as LC-NMR and/or LC-MS. [6] One of the most efficient and powerful tools for on-line isolation and identification of compounds in complex mixtures in the pharmaceutical industry is the LC-SPE- NMR system. In this study, LC- SPE/CRYO NMR technique was used for impurity profiling of novel azithromycin conjugates.

LC-SPE-NMR, azithromycin, impurities

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