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Sinteza piridinostilbenskih zaviralcev ligaz Mur = Synthesis of pyridinostilbene inhibitors of Mur ligases : Uniform Master's Study Programme PharmacyVerbič, KlaraOdpornost bakterij na protibakterijske učinkovine postaja vse večji zdravstveni problem. Glavna razloga za to sta neustrezna uporaba protibakterijskih učinkovin in upočasnjen razvoj novih ... protibakterijskih učinkovin. Zaradi tega sta potrebna razvoj in sinteza novih protibakterijskih učinkovin. V raziskavah se je pokazalo, da predstavljajo encimi, ki sodelujejo v znotrajceličnih stopnjah biosinteze peptidoglikana, velik potencial za razvoj novih učinkovin. V magistrski nalogi smo raziskovali sinteze novih piridinostilbenskih zaviralcev od ATP odvisnih ligaz MurC-F, ki katalizirajo pripajanje peptidov na peptidno verigo prekurzorja peptidoglikana. Zaviralce smo načrtovali na osnovi strukture že znanega zaviralca, ki so ga pri testiranju knjižnice protein kinaznih zaviralcev na ligaze Mur odkrili raziskovalci na Fakulteti za farmacijo. Najprej smo zamenjali furanski obroč z različnimi aromatskimi fragmenti in sintetizirali pet novih zaviralcev MurC-F. Nato smo spremenili tetrazolni del molekule in pripravili še dva dodatna zaviralca MurC-F. Z zamenjavo furanskega fragmenta smo dobili zaviralec encimov MurC-F, ki je imel podobno delovanje kot izhodna spojina (spojina 4b). Tudi spojini 5 in 6, ki sta imeli spremenjen tetrazolni del, sta se izkazali kot dobra zaviralca ligaz MurC-F. Sintetizirane spojine so dobro izhodišče za nadaljnje sinteze in načrtovanje novih multiplih zaviralcev ligaz MurC-F.Type of material - master's thesis ; adult, seriousPublication and manufacture - Ljubljana : [K. Verbič], 2019Language - slovenianCOBISS.SI-ID - 4728689
Author
Verbič, Klara
Other authors
Hrast, Martina |
Knez, Damijan, farmacevt
Topics
Bakterijska rezistenca |
protibakterijske učinkovine |
piridinostilbenski zaviralci |
MurC-F |
odpornost bakterij |
sinteza spojin
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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Verbič, Klara | |
Hrast, Martina | 32036 |
Knez, Damijan, farmacevt | 36438 |
Source: Personal bibliographies
and: SICRIS
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