Sökning: "prodrugs"

Visar resultat 1 - 5 av 18 avhandlingar innehållade ordet prodrugs.

1. 1. In vivo Pharmacokinetics of Two New Thrombin Inhibitor Prodrugs : Emphasis on Intestinal and Hepatobiliary Disposition and the Influence of Interacting Drugs

   Författare :Elin Matsson; Hans Lennernäs; Lars Knutson; Ulf Eriksson; Kim Brouwer; Uppsala universitet; []
   Nyckelord :MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; Direct thrombin inhibitors; prodrugs; ximelagatran; AZD0837; erythromycin; ketoconazole; drug-drug interactions; hepatobiliary transport; biliary clearance; ATP-binding cassette; ABC transporters; solute carriers; SLC transporters; CYP3A4; Biopharmacy; Biofarmaci; Biopharmaceutics; Biofarmaci;

   Sammanfattning : Biliary excretion is an important elimination route for many drugs and metabolites. For such compounds, it is important to know the extent of excretion and drug exposure in the bile, e.g., for the risk assessment of drug interactions, liver toxicity and the effects of genetic variants. LÄS MER

3. 2. Role of Multiple Glutathione Transferases in Bioactivation of Thiopurine Prodrugs : Studies of Human Soluble Glutathione Transferases from Alpha, Kappa, Mu, Omega, Pi, Theta, and Zeta Classes

   Författare :Birgitta I. Eklund; Bengt Mannervik; Mikael Widersten; Ralf Morgenstern; Uppsala universitet; []
   Nyckelord :Biochemistry; Glutathione Transferases; Thiopurines; Prodrug; Bioactivation; Screening Method; Chemotherapy; Functional plasticity; Modulated activity; Biokemi;

   Sammanfattning : A screening method was developed for identification of catalytically active enzymes in combinatorial cDNA libraries of mutated glutathione transferase (GST) derivatives expressed in E. coli. The method is based on spraying monochlorobimane (MCB) directly over bacterial colonies growing on agar. LÄS MER

4. 3. Galiellalactone Synthetic Studies

   Författare :Zilma Escobar; Centrum för analys och syntes; []
   Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; natural product; galiellalactone; prostate cancer; STAT3.;

   Sammanfattning : In search for remedies and treatments, science has recurred to Mother Nature. This is where galiellalactone was found, a fungal metabolite isolated from Galiella rufa in 1990. Since then chemists and biologists have been studying its properties and found it to be a potential candidate against castration-resistance prostate cancer (CRPC). LÄS MER

5. 4. Structural and functional studies of enzymes in nucleotide metabolism : a detailed investigation of two enzymes and interaction profiling of FDA-approved nucleoside analog drugs with 23 enzymes

   Författare :Louise Egeblad; Sveriges lantbruksuniversitet; Sveriges lantbruksuniversitet; []
   Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; NATURVETENSKAP; NATURAL SCIENCES; MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES;

   Sammanfattning : Enzymes in nucleotide metabolism serve as the producers of the building blocks for DNA and RNA. From a medical perspective, nucleotide metabolism, and in particular salvage pathway enzymes, have attracted special interest, as nucleoside prodrugs given in the treatment of cancer and HIV are converted into their active metabolite forms by these enzymes. LÄS MER

7. 5. Nucleoside phosphoramidates and related compounds : development of synthetic methods based on H-phosphonate chemistry

   Författare :Inger Kers; Wojciech J. Stec; Stockholms universitet; []
   Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; Organic Chemistry; organisk kemi;

   Sammanfattning : In this thesis, studies directed towards development of new synthetic methods for the preparation of nucleotide analogues of potential medical value as antisense, antigene or antiviral agents, are described.Two methods for synthesis of N3'->P5' and P3'->N5' phosphoramidate analogues with the nitrogen atom in bridging position of the internucleotide linkage was developed. LÄS MER