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NMR methods for studying structure and interactions of macrozones

Macrozones are novel, bioactive macrolide derivatives, conjugates of azithromycin and thiosemicarbazone. Macrolides, such as azithromycin are group of antibiotics which are active against Gram positive and some Gram negative bacteria. They exert their biological activity by binding to the 50S ribosome subunit. Due to the frequent and improper use of drugs bacterial resistance has emerged. There is a need to discover new, more effective antibiotics. In this work, three classes of macrozones were synthesized and characterized by NMR spectroscopy. In order to investigate mechanisms of macrozones activity, interactions with E. Coli ribosome were studied by trNOESY and STD NMR methods. Since 3D structure plays a significant role in bioactivity, free and bound state conformations of macrozones were also investigated. These results should contribute to discover and design new compounds with improved antibacterial activity.

azithromycin, biological activity, resistance, macrozones, spectroscopy NMR

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