dc.date.accessioned | 2013-03-12T08:53:21Z | |
dc.date.available | 2013-03-12T08:53:21Z | |
dc.date.issued | 2004 | en_US |
dc.date.submitted | 2004-12-20 | en_US |
dc.identifier.citation | Olberg, Dag Erlend. Protein binding prodrugs. Masteroppgave, University of Oslo, 2004 | en_US |
dc.identifier.uri | http://hdl.handle.net/10852/12083 | |
dc.description.abstract | A novel series of 5 -O-ester prodrugs of the anti-HIV drug 2 ,3 -dideoxyinosine (ddI,didanosine)
were synthesized for the purpose of increasing protein binding. Hope was that these derivates
would exhibit superior pharmacodynamic and pharmacokinetic properties against HIV-infection
than the parent drug, didanosine.
Ten compounds were synthesized, five fatty acid derivates and five dicarboxylic acid monoester
derivates. The fatty acid- and dicarboxylic acid derivates had the same carbon chain length.
Chain lengths were 4, 6, 8 ,12 and 16. The substances were tested for their protein binding ability
in a 4 % bovine serum albumin (BSA) solution using ultrafiltration. Two of the derivates, 5 -
dodecanedioic acid-(2 ,3 -dideoxyinosine)-monoester (C12) and 5 -hexadecanedioic-(2 ,3 -
dideoxyinosine)-monoester (C16) showed high affinity for albumin. The two derivates
demonstrated a protein binding of 95% and 100%, respectively. The parent compound, ddI,
had a protein binding of <5 % originally. The fatty acid and dicarboxylic acid derivate with a
eight carbon chain were tried displaced with octanoic acid (C8), oxazepam and warfarin. The
displacement studies indicated that there are common binding sites for the C8 derivates and the
displacers. | nor |
dc.language.iso | eng | en_US |
dc.subject | medisink kjemi proteinbinding HIV didanosine prodrug fettsyrer | en_US |
dc.title | Protein binding prodrugs : Synthesis and protein binding studies of didanonsine derivates | en_US |
dc.type | Master thesis | en_US |
dc.date.updated | 2005-12-14 | en_US |
dc.creator.author | Olberg, Dag Erlend | en_US |
dc.subject.nsi | VDP::568 | en_US |
dc.identifier.bibliographiccitation | info:ofi/fmt:kev:mtx:ctx&ctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:dissertation&rft.au=Olberg, Dag Erlend&rft.title=Protein binding prodrugs&rft.inst=University of Oslo&rft.date=2004&rft.degree=Masteroppgave | en_US |
dc.identifier.urn | URN:NBN:no-11411 | en_US |
dc.type.document | Masteroppgave | en_US |
dc.identifier.duo | 23380 | en_US |
dc.contributor.supervisor | Jo Klaveness | en_US |
dc.identifier.bibsys | 042462983 | en_US |