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Sinteza novih fosfinatnih deritavov L-alanil-D-glutaminske kisline = Synthesis of new phoshinate derivatives of L-alanyl-D-glutamic acid : diplomska nalogaGrbac, AlenkaV uvodu smo predstavili bakterijsko celièno steno, zgradbo in biosintezo peptidoglikana, encim MurD ter nekatere inhibitorje encima MurD. Peptidoglikanje najpomembnejsi sestavni del bakterijske ... stene, saj s svojo strukturo zagotavlja prezivetje bakterije v hipotoniènem okolju. Pri biosintezi peptidoglikana ima pomembno vlogo encim MurD, ki katalizira pripajanje D-glutaminske kisline na UDP-MurNAc-L-Ala. Ker D-aminokisline najdemo samo v prokariontih predstavlja encim MurD dobro selektivno tarèno mesto za naèrtovanje potencialnih protibakterijskih uèinkovin. V okviru diplomske naloge smo si za spojino vodnico izbrali spojino, ki je bila dober inhibitor encima MurD. Nas namen je bil izboljsati aktivnost spojine vodnice znaèrtnimi modifikacijami njene srukture (spojina ima fosfinatno vez, alaninski preostanek in para-nitrobenzilsulfonilno skupino na dusiku). Alaninski preostanek smo zamenjali z valinskim, leucinskim in izoleucinskim, spreminjali pa smo tudi polozaj nitro skupine na aromatskem obroèu. Na podlagiteh sprememb smo uspesno sintetizirali sedem novih fosfinatnih derivatov L-alanil-D-glutaminske kisline (8a, 8b, 9, 17b, 25a, 25b in 27). Sintetiziranim spojinam so izmerili sposobnost inhibicije encima MurD v standardnem encimskem testu. Kot najboljsa inhibitorja encima MurD sta se izkazali spojini 8b (spojina, ki ima valinski preostanek in meta-nitrobenzilsulfonilno skupino na dusiku) in 17b (spojina, ki ima leucinski preostanek in meta-nitrobenzilsulfonilno skupino na dusiku).Type of material - undergraduate thesisPublication and manufacture - Ljubljana : [Grbac, A.], 2003Language - slovenianCOBISS.SI-ID - 1394801
Author
Grbac, Alenka
Other authors
Gobec, Stanislav, 1970- |
Štrancar, Katja |
Mrhar, Aleš |
Planinšek, Odon
Topics
encim MurD |
inhibitorji |
metabolizem |
sinteza |
metode |
biološki testi
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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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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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DRS, in which the journal is indexed
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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Grbac, Alenka | ![]() |
Gobec, Stanislav, 1970- | 15284 |
Štrancar, Katja | 21458 |
Mrhar, Aleš | 06086 |
Planinšek, Odon | 14935 |
Source: Personal bibliographies
and: SICRIS
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