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Sinteza nekaterih metil 1-aril-3-hidroksi-1H-pirazol-4-karboksilatov
ID Jurajevčič, Manca (Author), ID Svete, Jurij (Mentor) More about this mentor... This link opens in a new window

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Abstract
V diplomskem delu sem se ukvarjala s sintezo spojin, pirazolovih derivatov, ki so že bili preučevani kot potencialni antimalariki. Spojine sem pripravila po postopku iz literature. Uspešno sem pripravila hidrazide metil malonata iz metil malonil klorida in derivatov hidrazina, kar sem potrdila z IR in NMR spektroskopijo. V drugi stopnji sem dobljene hidrazide kondenzirala z amid acetalom in jih nato ciklizirala v pirazole. S pomočjo IR in NMR spektroskopije sem dokazala, da sem uspešno sintetizirala želene produkte. Testirali smo biološko aktivnost produktov s standardiziranimi encimskimi testi, ki pa so na žalost pokazali, da spojine nimajo pričakovanega inhibitornega učinka na encim PfDHODH.

Language:Slovenian
Keywords:antimalariki, pirazoli, inhibitorji PfDHODH, encimski testi
Work type:Bachelor thesis/paper
Typology:2.11 - Undergraduate Thesis
Organization:FKKT - Faculty of Chemistry and Chemical Technology
Year:2022
PID:20.500.12556/RUL-139098 This link opens in a new window
COBISS.SI-ID:122287107 This link opens in a new window
Publication date in RUL:30.08.2022
Views:739
Downloads:71
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Secondary language

Language:English
Title:Synthesis of some methyl 3-hydroxy-1-phenyl-1H-pyrazole-4-carboxylates
Abstract:
In diploma work, I dealt with the synthesis of compounds, pyrazole derivatives, which have already been studied as potential antimalarials. I prepared the compounds according to the procedure from the literature. I successfully prepared methyl malonate hydrazide derivates from methyl malonyl chloride and hydrazine derivatives, which was confirmed by IR and NMR spectroscopy. In the second step, I condensed the obtained hydrazides with amide acetal and then cyclized them into pyrazoles. Using IR and NMR spectroscopy, I proved that I had successfully synthesized the desired products. We tested the biological activity of the products with standardized enzyme tests, which unfortunately showed that the compounds did not have the expected inhibitory effect on the PfDHODH enzyme.

Keywords:antimalarials, pyrazoles, inhibitors PfDHODH, enzyme tests

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