
<oai_dc:dc xmlns:dc="http://purl.org/dc/elements/1.1/" xmlns:oai_dc="http://www.openarchives.org/OAI/2.0/oai_dc/">
  <dc:identifier>https://phaidrabg.bg.ac.rs/o:17453</dc:identifier>
  <dc:identifier>cobiss:49966863</dc:identifier>
  <dc:identifier>thesis:5707</dc:identifier>
  <dc:language>srp</dc:language>
  <dc:date>2018</dc:date>
  <dc:subject xml:lang="eng">OSNO - Opšta sistematizacija naučnih oblasti, Farmaceutska hemija</dc:subject>
  <dc:subject xml:lang="srp">OSNO - Opšta sistematizacija naučnih oblasti, Farmaceutska hemija</dc:subject>
  <dc:subject xml:lang="srp">derivati 1,2-etandiamin-N,N&apos;-di-2-(3-cikloheksil)propanskekiseline, derivati 1,3-propandiamin-N,N&apos;-di-2-(3-cikloheksil)propanske kiseline,bioanalitička metoda, tečna hromatografija pod ultra visokim pritiskom u sprezisa masenom spektrometrijom (UHPLC-MS/MS), rastvorljivost, lipofilnost,membranska permeabilnost, docking, ADME(T) predviđanje, predviđanjemetaboličkih reakcija i metabolita - Metabolizer</dc:subject>
  <dc:subject xml:lang="eng">derivatives of (S,S)-1,2-ethanediamine-N,N&apos;-di-2-(3-cyclohexyl)propanoic acid and (S,S)-1,3-propanediamine-N,N&apos;-di-2-(3-cyclohexyl)propanoic acid, bioanalytical method, ultra-high performance liquidchromatography tandem mass spectrometry-UHPLC-MS/MS), solubility,lipophilicity, membrane permeability, docking study, ADME(T) prediction,prediction of metabolic reactions and metabolites - Metabolizer</dc:subject>
  <dc:subject xml:lang="srp">547.415.1:[543.544.5:004.94(043.3)</dc:subject>
  <dc:rights>http://creativecommons.org/licenses/by-nc-nd/2.0/at/legalcode</dc:rights>
  <dc:contributor>Marković, Bojan, 1978-</dc:contributor>
  <dc:contributor>Vladimirov, Sote, 1951-</dc:contributor>
  <dc:contributor>Sabo, Tibor, 1958-</dc:contributor>
  <dc:contributor>Stojisavljević Šatara, Svjetlana</dc:contributor>
  <dc:contributor>Dobričić, Vladimir</dc:contributor>
  <dc:type>info:eu-repo/semantics/bachelorThesis</dc:type>
  <dc:creator>Tubić, Biljana K., 1974-</dc:creator>
  <dc:title xml:lang="srp">Derivati etilendiamin-N,N&apos;-di-2-(3-cikloheksil) propanske kiseline sa potencijalnim citotoksičnim dejstvom - in silico/in vitro fizičko-hemijska i ADME karakterizacija : doktorska disertacija</dc:title>
  <dc:description xml:lang="srp">Estri (S,S)-1,2-etandiamin-N,N&apos;-di-2-(3-cikloheksil)propanske kiseline
(EDCP) sa metanolom (DM-EDCP), etanolom (DE-EDCP), propanolom (DPEDCP),
butanolom (DB-EDCP) i izobutanolom (DIB-EDCP) i estri (S,S)-1,3-
propandiamin-N,N&apos;-di-2-(3-cikloheksil)propanske kiseline (PDCP) sa
metanolom (DM-PDCP), etanolom (DE-PDCP), propanolom (DP-PDCP),
butanolom (DB-PDCP), izobutanolom (DIB-PDCP), pentanolom (DPE-PDCP) i
izopentanolom (DIPE-PDCP) dizajnirani su kao ligandi za Pt(IV) komplekse. U
in vitro ispitivanjima utvrđena je značajna citotoksična aktivnost za navedene
komplekse, ali i za ligande u nevezanom obliku. Ispitivana supstanca DE-EDCP
pokazala je najveću citotoksičnu aktivnost.
U ovoj doktorskoj disertaciji opisan je razvoj i validacija savremene
bioanalitičke metode - ultra visoko efikasne tečne hromatografije u sprezi sa
masenom detekcijom (UHPLC-MS/MS). Metoda je razvijena i validirana za
potrebe pretkliničkih ispitivanja, odnosno za određivanje ispitivane supstance
DE-EDCP u biološkom materijalu, kao i njenog potencijalnog metabolita EDCP.
Kao interni standard primenjen je strukturni analog DB-PDCP.
Tokom in vitro fizičko-hemijske biofarmaceutske karakterizacije ispitivanih
supstanci određena je i ocenjena njihova rastvorljivost u vodenom rastvoru,
lipofilnost i permeabilnost na veštačkim membranama. Profili rastvorljivosti
kiselina i njihovih estara se značajno razlikuju, dok su profili rastvorljivosti obe
kiseline (EDCP i PDCP) slični, kao i profili rastvorljivosti svih estara. Kiseline se
dobro rastvaraju u izrazito kiseloj sredini i u izrazito baznoj sredini, dok je
rastvorljivost estara najveća u izrazito kiseloj sredini...</dc:description>
  <dc:description xml:lang="eng">Esters of (S,S)-1,2-ethanediamine-N,N&apos;-di-2-(3-cyclohexyl)propanoic acid
(EDCP) with methyl alcohol (DM-EDCP), ethyl alcohol (DE-EDCP), n-propyl
alcohol (DP-EDCP), n-butyl-alcohol (DB-EDCP) and isobutyl-alcohol (DIBEDCP),
and esters of (S,S)-1,3-propanediamine-N,N&apos;-di-2-(3-
cyclohexyl)propanoic acid (PDCP) with methyl alcohol (DM-PDCP), ethyl
alcchol (DE-PDCP), n-propyl alcohol (DP-PDCP), n-butyl alcohol (DB-PDCP),
and isobutyl alcohol (DIB-PDCP), n-pentyl alcohol (DPE-PDCP) and isopentyl
alcohol (DIPE-PDCP) were designed as ligand of Pt(IV) complexes. During the in
vitro investigation it was found significantly cytotoxic activity of these
complexes, and also it was found cytotoxic activity of ligand without complexes.
Investigated substance DE-EDCP was exerted the strongest cytotoxic activity.
In this doctoral dissertation, there is presented a development and validation
of a new ultra-high-performance liquid chromatography tandem mass
spectrometry bioanalytical method (UHPLC-MS/MS). The developed method is
supposed for determination of DE-EDCP and its potential metabolit EDCP in
biological materials during non-clinical and clinical studies. The structural
analogue DB-PDCP was used as an internal standard.
During the in vitro biopharmaceutical characterization of the investigated
substances, there was performed a determination of solubility, lipophilicity and
membrane permeability. Profiles of solubility of the observed acids and their
corresponding esters are significantly different, while the profiles of solubility for
two acids (EDCP and PDCP) are similar as well as the profiles of solubility for all
the esters...</dc:description>
  <dc:description xml:lang="srp">Farmacija - Farmaceutska-medicinska hemija i strukturna analiza / Pharmacy- Pharmaceutical-medicinal chemistry and structural analysis  Datum odbrane: 09.03.2018. </dc:description>
  <dc:format>201 list</dc:format>
  <dc:format>6894405 bytes</dc:format>
</oai_dc:dc>