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Priprava, karakterizacija i biološka aktivnost makrozona, novih derivata azitromicina
Zagreb: University of Zagreb, Faculty of Science, 2022. urn:nbn:hr:217:942141
Mikulandra, Ivana
University of Zagreb
Faculty of Science
Department of Chemistry

Institutional repository: Repository of the Faculty of Science

Cite this document

Mikulandra, I. (2022). Priprava, karakterizacija i biološka aktivnost makrozona, novih derivata azitromicina (Doctoral thesis). Zagreb: University of Zagreb, Faculty of Science. Retrieved from https://urn.nsk.hr/urn:nbn:hr:217:942141

Mikulandra, Ivana. "Priprava, karakterizacija i biološka aktivnost makrozona, novih derivata azitromicina." Doctoral thesis, University of Zagreb, Faculty of Science, 2022. https://urn.nsk.hr/urn:nbn:hr:217:942141

Mikulandra, Ivana. "Priprava, karakterizacija i biološka aktivnost makrozona, novih derivata azitromicina." Doctoral thesis, University of Zagreb, Faculty of Science, 2022. https://urn.nsk.hr/urn:nbn:hr:217:942141

Mikulandra, I. (2022). 'Priprava, karakterizacija i biološka aktivnost makrozona, novih derivata azitromicina', Doctoral thesis, University of Zagreb, Faculty of Science, accessed 23 November 2024, https://urn.nsk.hr/urn:nbn:hr:217:942141

Mikulandra I. Priprava, karakterizacija i biološka aktivnost makrozona, novih derivata azitromicina [Doctoral thesis]. Zagreb: University of Zagreb, Faculty of Science; 2022 [cited 2024 November 23] Available at: https://urn.nsk.hr/urn:nbn:hr:217:942141

I. Mikulandra, "Priprava, karakterizacija i biološka aktivnost makrozona, novih derivata azitromicina", Doctoral thesis, University of Zagreb, Faculty of Science, Zagreb, 2022. Available at: https://urn.nsk.hr/urn:nbn:hr:217:942141

Metadata
TitlePriprava, karakterizacija i biološka aktivnost makrozona, novih derivata azitromicina
Title (english)Preparation, characterization and biologial activity of macrozones, new azithromycin derivatives
AuthorIvana Mikulandra
MentorPredrag Novak (mentor)
Committee memberVesna Petrović-Peroković (predsjednik povjerenstva)
Committee memberDražen Vikić-Topić (član povjerenstva)
Committee memberIvo Piantanida (član povjerenstva)
GranterUniversity of Zagreb
Faculty of Science
(Department of Chemistry)
Zagreb
Defense date and country2022-06-14, Croatia
Scientific / art field,
discipline and subdiscipline		NATURAL SCIENCES
Chemistry
Universal decimal classification
(UDC)		54 - Chemistry. Crystallography. Mineralogy
Abstract
Značajan porast bakterijske rezistencije utječe na sve veću potrebu za istraživanjem i razvojem novih antibiotika. U sklopu ovog rada pripravljene su tri nove klase makrozona, konjugata makrolidnog antibiotika azitromicina i tiosemikarbazona. Tiosemikarbazoni su korišteni za kemijsku modifikaciju azitromicina na tri različita položaja. Cilj rada je priprava novih derivata makrolida sa širim spektrom biološke aktivnosti. Pripravljenim spojevima određena je biološka aktivnost in vitro na susceptibilne i rezistentne Gram-pozitivne i Gram-negativne bakterije te su istražene interakcije s biološkim receptorima. Za proučavanje interakcija primijenjena je spektroskopija NMR, cirkularni dikroizam, fluorescencijska spektroskopija i molekulsko modeliranje. Makrozoni su pokazali zadovoljavajuću biološku aktivnost, posebice na neke rezistentne bakterijske sojeve na koje azitromicin nije aktivan. Rezultati dobiveni spektroskopskim metodama i molekulskim modeliranjem ukazuju na odnos strukture i aktivnosti novih derivata azitromicina, što može poslužiti za dizajn i otkriće biaktivnijih derivata makrolida.
Abstract (english)
Owing to a significant increase in bacterial resistance, a high need for discovery and development of new antibiotics has emerged. As part of this work, three novel classes of macrozones, conjugates of macrolide antibiotic azithromycin and thiosemicarbazones, were prepared. Thiosemicarbazones were used to chemically modify azithromycin at three different positions. The aim of this thesis was to prepare compounds with a wider range of biological activity including resistant bacterial strains. In vitro biological activity of the prepared compounds was determined against susceptible and resistant Gram-positive and Gram-negative bacteria, and interactions with biological receptors were investigated. Macrozones showed satisfactory biological activity, especially against some resistant bacterial strains to which azithromycin is inactive. NMR spectroscopy, circular dichroism, fluorescence spectroscopy, and molecular modeling were further used to study interactions of selected compounds with biological targets. The results obtained by spectroscopic methods and molecular modeling indicate a relationship between structure and activity of new azithromycin derivatives, which can be used for design and discovery of more active macrolide derivatives.
Keywords
Keywords (english)
Languagecroatian
URN:NBNurn:nbn:hr:217:942141
Promotion2022
ProjectNumber: 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 programmeTitle: Doctoral study in chemistry
Study programme type: university
Study level: postgraduate
Academic / professional title: doktor/doktorica znanosti, područje prirodnih znanosti, polje kemija (doktor/doktorica znanosti, područje prirodnih znanosti, polje kemija)
Type of resourceText
Extent178 str. ; 30 cm
File originBorn digital
Access conditionsOpen access
Embargo expiration date: 2022-12-14
Terms of useLicence In copyright icon
Created on2022-06-20 13:31:52