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Sinteza in vrednotenje novih zaviralcev DNA-giraze B z N-(benzo[d]tiazol-2-il)-1H-pirol-2-karboksamidnim strukturnim delom = Synthesis and evaluation of new DNA gyrase B inhibitors with the N-(benzo[d]thiazol-2-yl)-1H-pyrrole-2-carboxamide structural part : magistrska naloga : enoviti magistrski študijski program FarmacijaFridrih, NinaOdkritju večine pomembnejših skupin protibakterijskih učinkovin sredi 20. stoletja danes sledi zaskrbljujoča grožnja obdobja bakterijske odpornosti. Za premagovanje ovir pri razvoju nujno potrebnih ... novih protibakterijskih učinkovin znanstveniki raziskujejo nove molekularne tarče ali učinkovine, ki bi delovale na znane tarče preko novih mehanizmov delovanja. Ene izmed dobro uveljavljenih tarč so bakterijske topoizomeraze, kamor spadata tudi encima DNA-giraza in topoizomeraza IV. DNA-giraza in topoizomeraza IV imata pri podvajanju molekule DNA pomembno vlogo. Oba sta heterotetramerna encima, sestavljena iz dveh parov podenot: DNA-giraza iz dveh podenot GyrA in dveh podenot GyrB, topoizomeraza IV pa iz dveh podenot ParC in dveh podenot ParE. Podenoti GyrA in GyrB sta po aminokislinskem zaporedju podobni podenotam ParC in ParE. Zaradi strukturne podobnosti obstaja možnost načrtovanja učinkovin, ki zavirajo oba encima hkrati. Glavna funkcija GyrA/ParC je razcepitev in združitev molekule DNA med podvajanjem, energijo za ta proces pa zagotavlja GyrB/ParE s hidrolizo ATP. S pomočjo kristalnih struktur kompleksov DNA-giraze B z znanimi zaviralci smo načrtovali in pripravili 7 novih potencialnih ATP-kompetitivnih zaviralcev DNA-giraze B. Sintetiziranim spojinam je skupen N-(benzo[d]tiazol-2-il)-1H-pirol-2-karboksamidni del molekule. Spojine smo testirali na encimu DNA-giraza iz Escherichia coli, dve pa še na DNA-girazi bakterije Staphylococcus aureus ter na DNA topoizomerazi IV bakterije E. coli in S. aureus. Spojinam, ki so pokazale dobro aktivnost na encimih smo določili še protibakterijsko aktivnost na bakterijskih sevih Acinetobacter baumannii, E. coli, Enterobacter aerogenes, Enterococcus faecalis, Enterococcus faecium, Klebsiella pneumoniae, Pseudomonas aeruginosa in S. aureus. Na encimskih in protibakterijskih testiranjih se je kot najbolj aktivna izkazala spojina 16, s srednjo zaviralno koncetracijo (IC50) 13,4 nM na DNA-girazo iz E. coli, ki ima v svoji strukturi 3,4-dikloro-5-metil-1H-pirolamidni fragment in prosto karboksilno kislino na desni strani molekule. Spojine 16 je imela zelo dobro aktivnost tudi na DNA-girazi iz S. aureus ter topoizomerazi IV iz E. coli in S. aureus, na protibakterijskem testiranju pa je dosegla zelo nizke minimalne zaviralne koncentracije (MIK90) proti bakterijam S. aureus (MIK90 = 1,56 microM), E. coli (MIK90 = 12,5 microM), E. faecalis (MIK90 = 0,39 microM), E. faecium (MIK90 = 0,56 microM) in A. baumannii (MIK90 = 6,25 microM).Type of material - master's thesis ; adult, seriousPublication and manufacture - Ljubljana : [N. Fridrih], 2019Language - slovenianCOBISS.SI-ID - 4743281
Author
Fridrih, Nina
Other authors
Zidar, Nace
Topics
Bakterijska rezistenca |
protibakterijska učinkovina |
ATP-kompetitivni zaviralci |
DNA giraza B |
topoizomeraze |
mehanizmi odpornosti
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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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Fridrih, Nina | ![]() |
Zidar, Nace | 28905 |
Source: Personal bibliographies
and: SICRIS
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