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LC-SPE/NMR analysis of macrozones, new bioactive azithromycin conjugates

Azithromycin belongs to an azalide subclass of 15- membered macrolide antibiotics. With a much improved pharmacokinetic and therapeutic properties over erythromycin, azithromycin became the most widely used broad-spectrum antibiotic. [1] An increasing number of antibiotic-resistant bacteria, especially respiratory tract pathogens, demand a more effective antimicrobial agents to be synthesized.[2] Thiosemicarbazones belong to a large group of thiourea derivatives and are well known as antibacterial, antiviral, anti- inflammatory, antifungal and anticancer therapeutics.[3] Conjugation of the azithromycin analogue, 9a- (γ-aminopropyl) derivative, and thiosemicarbazone moieties resulted in novel compounds, macrozones, which showed good in vitro activity against selected Gram positive and Gram negative bacterial strains. Modern approach to the impurity profiling of bioactive compounds is based on the use of hyphenated systems, such as LC-NMR and/or LC- MS.[4-6] 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.[6-7] In this study, LC-SPE/NMR technique was used for impurity profiling of the novel macrozones.

macrozones, azithromycin, thiosemicarbazides, synthesis

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