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Sinteza etilaminskih zaviralcev bakterijske giraze kot novih protimikrobnih učinkovin = Synthesis of ethylamine inhibitors of bacterial gyrase as new antimicrobial agents : enoviti magistrski študij farmacijaAdamlje, BoštjanProtimikrobne učinkovine so pomemben razred učinkovin, saj preprečujejo številne smrti, povzročene z bakterijskimi okužbami, ki kljub temu ostajajo eden vodilnih vzrokov umrljivosti po celem svetu. ... Glavni problem protimikrobne terapije je namreč pojav rezistentnih sevov bakterij zaradi nepravilne rabe protimikrobnih učinkovin, poleg tega na trg prihaja vedno manj novih učinkovin. Glede na mehanizem delovanja poznamo več skupin učinkovin, ena izmed pomembnih tarč protimikrobnih učinkovin je tudi giraza B. V okviru eksperimentalnega dela smo sintetizirali nove zaviralce, ki delujejo na način, da tekmujejo za vezavno mesto z ATP. Pripravili smo zaviralce z benzotiazolnim ogrodjem, na katerega smo na mesto 2, kjer se nahaja aminska funkcionalna skupina, pripeli 3,4-dikloro-5-metilpirol, na amidno ali fenolno funkcionalno skupino pa smo pripeli etanaminski distančnik. V sklopu sinteze smo uporabljali različne analitske tehnike, kot so tekočinska kromatografija, sklopljena z masnim spektrometrom in tankoplastna kromatografija. Strukturo smo dokončno potrdili z jedrsko magnetno resonanco. Prvotno zastavljene sintezne poti preko N-alkiliranja benzotiazola niso dale željene spojine, zato smo poiskali ustrezne alternative. Za ustrezno se je izkazala nukleofilna aromatska substitucija z Boc zaščitenim etandiaminom in p-fluoronitro benzenom, sledilo je acetiliranje, redukcija nitro skupine in ciklizacija do željenega produkta. Na koncu smo uspešno izolirali le eno končno spojino.Type of material - master's thesis ; adult, seriousPublication and manufacture - Ljubljana : [B. Adamlje], 2023Language - slovenianCOBISS.SI-ID - 165204739
Author
Adamlje, Boštjan
Other authors
Ilaš, Janez
Topics
Protimikrobna zdravila |
pirol |
benzotiazoli |
zaviralci giraze B |
protimikrobne učinkovine |
DNA topoizomeraze |
sinteza terc-butil karbamata

Library/institution |
City | Acronym | For loan | Other holdings |
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Faculty of Pharmacy, Ljubljana | Ljubljana | FFALJ |
reading room 1 cop.
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Adamlje, Boštjan | ![]() |
Ilaš, Janez | 24400 |
Source: Personal bibliographies
and: SICRIS
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