engleski

Synthesis, structure characterization and interactions of 4“-aminopropyl derivative of azithromycin

Azithromycin belongs to macrolide class of antibiotics wich exert its biological activity by binding to bacterial ribosome at or near the peptidyl transferase center thus inhibiting protein biosynthesis. They are effective in treating infections caused by Gram-positive and some Gram-negative bacteria. Due to the increased development of bacterial resistance much effort is directed towards the discovery of new more potent antibiotics. A series of bioactive azithromycin derivatives, the new class of macrozones have been prepared by coupling thiosemicarbazones to azithromycin at position 4" (Figure 1). Here we present their synthesis, characterization and interactions of macrozone precursor, 4"-aminopropyl azithromycin with the ribosome isolated from E. Coli. A combination of NMR experiments such as saturation transfer difference (STD) and transferred nuclear Overhauser effect spectroscopy (trNOESY) and molecular modeling were applied to determine binding epitopes and explore bound conformations.

macrozones ; synthesis ; structure ; characterization

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