Interakcije 4"-benzil-makrozona i njegova kompleksa s niklom(II) s biološkim metama tehnikama STD i WaterLOGSY NMR

master's thesis

• Title (english): Interactions of benzyl-4"-macrozone and its nickel(II) complex with biological targets by STD and WaterLOGSY NMR techniques
• Author: Kristina Delaš
• Mentor: Predrag Novak (mentor)
• Committee member: Predrag Novak (predsjednik povjerenstva)
• Committee member: Ivana Biljan (član povjerenstva)
• Committee member: Mirta Rubčić (član povjerenstva)
• Committee member: Tomislav Jednačak (član povjerenstva)
• Granter: University of Zagreb; Faculty of Science; (Department of Chemistry); Zagreb
• Defense date and country: 2024-02-21, Croatia
• Scientific / art field, discipline and subdiscipline: NATURAL SCIENCES; Chemistry

Abstract

Povećana rezistencija patogenih bakterija na dosad poznate lijekove i nedostatak razvoja novih antibiotika predstavljaju globalni medicinski problem koji se može riješiti jedino otkrivanjem biološki aktivnih spojeva s izraženim antibakterijskim djelovanjem. Makrolidni antibiotici (makrolidi) imaju široki spektar djelovanja i učinkoviti su na većinu Gram-pozitivnih i Gram-negativnih bakterija. Jedan od najvažnijih predstavnika druge generacije makrolida je azitromicin. Povezivanjem azitromicina i nekih biološki aktivnih tiosemikarbazona dobiveni su njihovi konjugati makrozoni koji su pokazali povećanu učinkovitost i aktivnost na neke višestruko rezistentne sojeve bakterija. Biološka svojstva makrozona mogu se dodatno poboljšati kompleksiranjem s kationima prijelaznih metala. U ovom diplomskom radu istražena je aktivnost benzil-4''-makrozona i kompleksa nikla(II) s makrozonskim 4''- derivatom azitromicina. Interakcije pripravljenih spojeva s ribosomom izoliranim iz bakterije Escherichia coli i s goveđim albuminom iz seruma (BSA) određene su i analizirane pomoću tehnika STD i WaterLOGSY NMR te su određeni epitopi vezanja.

Abstract (english)

An increased resistance of pathogenic bacteria to previously known drugs and the lack of development of new antibiotics represent a global medical problem that can only be solved by discovering biologically active compounds with increased antibacterial activity. Macrolide antibiotics (macrolides) have a broad spectrum of activity and are effective against most Gram-positive and Gram-negative bacteria. One of the most important representatives of the second generation of macrolides is azithromycin. By linking azithromycin and some biologically active thiosemicarbazones, their conjugates, macrozones, were obtained, which showed increased efficiency and activity against some multi-resistant strains of bacteria. The biological properties of macrozones can be further improved by complexing with transition metal cations. In this thesis, the activity of benzyl-4''-macrozone and nickel(II) complex with macrozone 4''-derivative of azithromycin was investigated. The interactions of the prepared compounds with the ribosome isolated from the bacterium Escherichia coli and with bovine albumin (BSA) have been investigated and analysed by using STD and WaterLOGSY NMR techniques and binding epitopes have been determined.

• Keywords: azitromicin; makrolidni antibiotici; makrozoni; ribosom; STD NMR; WaterLOGSY NMR
• Keywords (english): azithromycin; macrolide antibiotics; macrozones; ribosome; STD NMR; WaterLOGSY NMR
• Language: croatian
• URN:NBN: urn:nbn:hr:217:884767
• Project: Number: IP-2018-01-8098; Title: Makrozoni, novi konjugati makrolidnih antibiotika: Dizajn, priprava i interakcije; Title: Macrozones, New Conjugates of Macrolide Antibiotics: Design, Synthesis and Interactions; Acronym: Makrozoni/Macrozones; Leader: Predrag Novak; Jurisdiction: Croatia; Funder: HRZZ; Funding stream: IP
• Study programme: Title: Graduate university studies in chemistry; specializations in: Graduate university studies in chemistry; Course: Graduate university studies in chemistry; Study programme type: university; Study level: graduate; Academic / professional title: sveučilišni/a magistar/magistra kemije (sveučilišni/a magistar/magistra kemije)
• Type of resource: Text
• File origin: Born digital
• Access conditions: Open access
• Created on: 2024-03-11 09:49:04