| Popis: |
Porast rezistencije bakterija na antibiotike koji su trenutno na tržištu potaknuo je potrebu za otkrivanjem novih. Makrolidni antibiotik azitromicin koristi se za liječenje bolesti uzrokovanih Gram-pozitivnim i Gram-negativnim bakterijama. Makrozoni su konjugati azitromicina i tiosemikarbazona pripremljeni za liječenje infekcija uzrokovanih rezistentnim bakterijama, s potencijalom zaobilaženja razvijenih mehanizama rezistencije. Kako bi se dodatno povećala biološka aktivnost i farmakološka svojstva, napravljeni su kompleksi tiosemikarbazona s metalnim ionima. U ovom radu prvo je pripravljen tiosemikarbazon izveden iz 4- aminobenzojeve kiseline i salicilaldehida. Nakon toga, dobiveni tiosemikarbazon je vezan na 4''-aminopropilni derivat azitromicina dajući pripadajući makrozon. Istražena je mogućnost kompleksiranja s ionima bakra(II) i nikla(II). Sintetizirani spojevi karakterizirani su spektroskopijom NMR. The increase in bacterial resistance to currently marketed antibiotics has prompted the need to discover new ones. The macrolide antibiotic azithromycin is used to treat diseases caused by Gram-positive and Gram-negative bacteria. Macrozones are conjugates of azithromycin and thiosemicarbazones prepared to treat infections caused by resistant bacteria, with potential of bypassing the developed resistance mechanisms. In order to further increase biological activity and pharmacological properties thiosemicarbazone complexes with metal ions have been made. In this work, a thiosemicarbazone derived from 4-aminobenzoic acid and salicylaldehyde was prepared first. Subsequently, the resulting thiosemicarbazone was bound to the 4''-aminopropyl derivative of azithromycin. The possibility of complexation with copper (II) and nickel (II) ions was explored. The synthesized compounds were characterized by NMR spectroscopy. |
