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master's thesis
Sinteza i karakterizacija hibrida artezunata i β-karbolina
Zagreb: University of Zagreb, Faculty of Pharmacy and Biochemistry, 2022. urn:nbn:hr:163:361755
Kravaršćan, Neva
University of Zagreb
Faculty of Pharmacy and Biochemistry
Department of medicinal chemistry

Institutional repository: Repository of Faculty of Pharmacy and Biochemistry University of Zagreb

Cite this document

Kravaršćan, N. (2022). Sinteza i karakterizacija hibrida artezunata i β-karbolina (Master's thesis). Zagreb: University of Zagreb, Faculty of Pharmacy and Biochemistry. Retrieved from https://urn.nsk.hr/urn:nbn:hr:163:361755

Kravaršćan, Neva. "Sinteza i karakterizacija hibrida artezunata i β-karbolina." Master's thesis, University of Zagreb, Faculty of Pharmacy and Biochemistry, 2022. https://urn.nsk.hr/urn:nbn:hr:163:361755

Kravaršćan, Neva. "Sinteza i karakterizacija hibrida artezunata i β-karbolina." Master's thesis, University of Zagreb, Faculty of Pharmacy and Biochemistry, 2022. https://urn.nsk.hr/urn:nbn:hr:163:361755

Kravaršćan, N. (2022). 'Sinteza i karakterizacija hibrida artezunata i β-karbolina', Master's thesis, University of Zagreb, Faculty of Pharmacy and Biochemistry, accessed 28 November 2024, https://urn.nsk.hr/urn:nbn:hr:163:361755

Kravaršćan N. Sinteza i karakterizacija hibrida artezunata i β-karbolina [Master's thesis]. Zagreb: University of Zagreb, Faculty of Pharmacy and Biochemistry; 2022 [cited 2024 November 28] Available at: https://urn.nsk.hr/urn:nbn:hr:163:361755

N. Kravaršćan, "Sinteza i karakterizacija hibrida artezunata i β-karbolina", Master's thesis, University of Zagreb, Faculty of Pharmacy and Biochemistry, Zagreb, 2022. Available at: https://urn.nsk.hr/urn:nbn:hr:163:361755

Metadata
TitleSinteza i karakterizacija hibrida artezunata i β-karbolina
Title (english)Synthesis and characterization of artezunate β-carboline hybrid
AuthorNeva Kravaršćan
MentorZrinka Rajić (mentor)
Committee memberZrinka Rajić (predsjednik povjerenstva)
Committee memberHrvoje Rimac (član povjerenstva)
Committee memberMaja Ortner Hadžiabdić (član povjerenstva)
GranterUniversity of Zagreb
Faculty of Pharmacy and Biochemistry
(Department of medicinal chemistry)
Zagreb
Defense date and country2022-08-30, Croatia
Scientific / art field,
discipline and subdiscipline		BIOMEDICINE AND HEALTHCARE
Pharmacy
Pharmacy
Abstract
Otkriće artemizina označilo je prekretnicu u terapiji malarije, čemu svjedoči preporuka SZO da se ACT koristi kao prva linija u liječenju ove bolesti. Međutim, pojava rezistentnih sojeva plazmodija ugrožava učinkovitost terapije, zbog čega je potrebno kontinuirano razvijati nove antimalarike. Jedan od pristupa u dizajniranju i razvoju novih lijekova je molekulska hibridizacija koja podrazumijeva povezivanje dvije biološki aktivne molekule u jedinstveni kemijski entitet, odnosno hibridnu molekulu. Racionalnim odabirom roditeljskih molekula moguće je pripraviti hibrid koji djeluje na različite mete zbog čega ostvaruje snažnije djelovanje te neće doći do razvoja rezistencije. U okviru ovog diplomskog rada pripravljen je hibrid artezunata, polusintetskog derivata artemizinina i harmina, β-karbolinskog alkaloida s izraženim antimalarijskim djelovanjem korištenjem reakcije povezivanja uz coupling reagens HATU i bazu DIEA (spoj 6). Za potrebe sinteze hibrida, sintetiziran je i amin 5, u pet reakcijskih koraka. Struktura konačnog spoja potvrđena je uobičajnim analitičkim i spektroskopskim metodama (IR, MS, 1H i 13C NMR). U nastavku istraživanja pripravljenom hibridu bit će ispitano antimalarijsko i protutumorsko djelovanje.
Abstract (english)
The discovery of artemisinin was a breakthrough in the treatment of malaria leading to the recommendation of the WHO to use ACT as the first-line therapy against malaria. Nevertheless, the occurrence of drug-resistant Plasmodium strains challenges its efficency and urges the need for constant development of new antimalarials. One of the approaches in the discovery of new bioactive agents is molecular hybridization, which represents synthesis of novel chemical entities (hybrid molecule) by forming covalent bond between two biologically active molecules. Rational selection of parent molecules enables the preparation of a hybrid with improved properties. Within this Master Thesis, hybrid (6) comprising artesunate, semisynthetic derivative of artemizinin and harmine, β-carboline alkaloid with pronounced antimalarial activity, was prepared by coupling reaction using HATU and DIEA. For the purpose of the hybrid synthesis, amine 5 was synthesized as well, through five reaction steps. The structure of novel compound was confirmed using standard analytical and spectroscopic methods (IR, MS, 1H i 13C NMR). Antimalarial and antiproliferative activity of the synthesized hybrid 6 will be evaluated in the future studies.
Keywords
Keywords (english)
Languagecroatian
URN:NBNurn:nbn:hr:163:361755
Study programmeTitle: Pharmacy
Study programme type: university
Study level: integrated undergraduate and graduate
Academic / professional title: magistar/magistra farmacije (magistar/magistra farmacije)
Type of resourceText
File originBorn digital
Access conditionsOpen access
Embargo expiration date: 2024-08-30
Terms of useLicence In copyright icon
Created on2022-09-05 13:57:06