NMR and fluorometric studies of bioactive macrozone interactions with their biological targets

Autor: Jednačak, Tomislav, Mikulandra, Ivana, Smokrović, Kristina, Kapustić, Monika, Delaš, Kristina, Piantanida, Ivo, Jurković, Marta, Zangger, Klaus, Novak, Predrag
Přispěvatelé: Bregović, Nikola, Namjesnik, Danijel, Novak, Predrag, Parlov Vuković, Jelena
Jazyk: angličtina
Rok vydání: 2023
Předmět:
Popis: Macrozones are new conjugates of azithromycin and thiosemicarbazones, which exhibit very good in vitro antibacterial activities against susceptible and some resistant bacterial strains thus showing a potential for further development. In this work, we applied a combination of NMR and fluorometric methods to study interactions of bioactive macrozones with their biological targets: bovine serum albumin and ribosome isolated from Escherichia coli. Saturation transfer difference (STD) and water-ligand observed via gradient spectroscopy (WaterLOGSY) spectra provided valuable data on ligand orientation, solvent exposure, binding epitopes and specificity. The binding stoichiometry and association constants were calculated from fluorometric data. These results can serve as a good starting point for the design of new macrozones and their metal complexes with improved bioactivity.
Databáze: OpenAIRE