Sinteza i karakterizacija urea harmina i aminoalkohola

master's thesis

• Title (english): Synthesis and characterization of urea harmines and aminoalcohols
• Author: Ines Jurak
• Mentor: Zrinka Rajić (mentor)
• Committee member: Zrinka Rajić (predsjednik povjerenstva)
• Committee member: Kristina Pavić (član povjerenstva)
• Committee member: Miranda Sertić (član povjerenstva)
• Granter: University of Zagreb; Faculty of Pharmacy and Biochemistry; (Department of medicinal chemistry); Zagreb
• Defense date and country: 2022-06-21, Croatia
• Scientific / art field, discipline and subdiscipline: BIOMEDICINE AND HEALTHCARE; Pharmacy; Pharmacy

Abstract

Harmin je β-karbolinski alkaloid prirodnog podrijetla koji je u mnogim istraživanjima pokazao brojne farmakološke učinke, uključujući i antimalarijsko djelovanje. Selektivnim inhibitornim djelovanjem na protein toplinskog šoka P. falciparum (PfHsp90) u in vitro i in vivo istraživanjima uspješno je djelovao na parazita P. falciparum. Zbog specifičnog mehanizma djelovanja i mogućeg sinergizma s drugim lijekovima postoji značajan potencijal za smanjenje rezistencije na postojeću terapiju, koja je postala globalni javnozdravstveni problem. U okviru ovog rada sintetizirana su dva nova spoja, uree harmina s aminoalkoholima u položaju 9 -karbolinskog prstena (5a,b). Novosintetiziranim spojevima potvrđena je struktura te su okarakterizirani analitičkim i spektroskopskim metodama koje uključuju IR, 1H NMR, 13C NMR te MS. Novim spojevima je također određena i temperatura tališta, a u kasnijim istraživanjima bit će im ispitano i antimalarijsko djelovanje.

Abstract (english)

Harmine is a naturally occurring β-carboline alkaloid which was proven to have many pharmacological effects, including antimalarial. Harmine exhibited activity against P. falciparum in in vitro and in vivo studies, possibly due to its selective and inhibitory effect on P. falciparum heat shock protein (PfHsp90). Because of the specific mechanism of action and synergy with other antimalarials, harmine possesses a potential for lowering the incidence of resistance to the available drugs, which has become a global health burden. In this thesis two novel compounds were synthesised, harmine ureas with amino alcohols, 5a and 5b. The newly synthesized compounds have been characterized using spectroscopic and analytical methods, (IR, 1H NMR, 13C NMR, MS) and their melting point was determined. Future research will focus on evaluation of their antimalarial activity.

• Keywords: harmin; urea; malarija; aminoalkohol; benzotriazol
• Keywords (english): harmine; urea; malaria; aminoalcohol; benzotriazole
• Language: croatian
• URN:NBN: urn:nbn:hr:163:766573
• Study programme: Title: Pharmacy; Study programme type: university; Study level: integrated undergraduate and graduate; Academic / professional title: magistar/magistra farmacije (magistar/magistra farmacije)
• Type of resource: Text
• File origin: Born digital
• Access conditions: Open access; Embargo expiration date: 2024-06-21
• Created on: 2022-07-21 13:52:08