Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 9 of 9 for “"Ester prodrugs"”.
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Novel Transporter Targeted Lipid Ester Prodrugs of Cidofovir and Sustained Release Formulations for Cytomegalovirus Infection
… we have tested novel transporter targeted lipid prodrugs of CDF and their nanoparticle formulations to achieve sustain drug delivery for the treatment of CMV retinitis. These prodrugs contains lipid linker of different carbon chain length (e.g. C2, C6, and C12) carrying minimum two functional …
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Targeting Mitochondrial ROS Production in Kidney Transplantation
… of this thesis was to determine whether malonate ester prodrugs, which competitively inhibit SDH, may reduce mitochondrial ROS production and ameliorate IRI in models of kidney transplantation. Herein, I show that the metabolic changes required for mitochondrial ROS production on reperfusion, …
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Ocular pharmacokinetics and efficacy of various amino acid and dipeptide prodrugs of ganciclovir
… of GCV. A series of dipeptide monoester prodrugs and amino acid monoester and diester prodrugs were designed to target the nutrient transporters peptide transporter (hPEPT1) and sodium dependent neutral and cationic transporter (B [super 0,+]), respectively. The overall objectives …
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The percutaneous absorption of ionisable compounds
… properties of this molecule, mono-, di- and tri-ester prodrugs were examined. These were assessed for stability and subsequent breakdown with respect to pH by HPLC. In vitro percutaneous absorption was observed using the triester, but not the ionic mono- or di-esters. The triester absorption …
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Preclinical pharmacokinetic evaluation of novel antimalarial and antituberculosis drug leads
… Investigation of two novel fusidic acid C-3 ester prodrugs aimed at repositioning fusidic acid for tuberculosis, showed high concentrations of the rodent specific 3-epifusidic acid metabolite that greatly reduced exposure of fusidic acid in mice. Further organ distribution studies showed a …
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Developing drugs to attenuate succinate accumulation and oxidation
… were selected for further development. Malonate ester prodrugs with different properties were characterised. Hydrolysis rates of the esters differed greatly, with tuned, labile, malonate esters releasing malonate much more rapidly. Malonate esters were taken up into cells and hydrolysed to …
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Synthesis, Physicochemical And Biopharmaceutical Characterisation Of Pro-Antibiotic Esters; Free Bases Of Ciprofloxacin
… dosing. This study was designed to synthesise esters of Ciprofloxacin, a model drug using alcohol co-formers (isopentanol, n-butanol and isobutanol) with a view to improving the physicochemical and biopharmaceutical properties of Ciprofloxacin. Three esters of ciprofloxacin were synthesised, …
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Synthesis, Physicochemical And Biopharmaceutical Characterisation Of Pro-Antibiotic Esters; Free Bases Of Ciprofloxacin
… dosing. This study was designed to synthesise esters of Ciprofloxacin, a model drug using alcohol co-formers (isopentanol, n-butanol and isobutanol) with a view to improving the physicochemical and biopharmaceutical properties of Ciprofloxacin. Three esters of ciprofloxacin were synthesised, …
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Investigating permeation of anti-mycobacterial agents in Mycobacterium tuberculosis and M. tuberculosis-infected macrophages in vitro as a model for early stage tuberculosis drug discovery
… (3-ketoFA or GKFA37), and two C-3 alkyl esters (GKFA16 and GKFA17) as FA prodrugs were utilized in the study. In addition, another chemical class, the less lipophilic benzoxazole-based oxime derivatives were also investigated. Moxifloxacin (MXF), levofloxacin (LVF), bedaquiline (BDQ), …