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 20 of 112 for “"Prodrugs"”.
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Towards Photoredox-Cleavable Prodrugs
… molecules from inactive precursors, e.g. prodrugs. Photouncaging is most often achieved through a direct release approach employing a chromophore as the photocaging group, which absorbs light and followingly undergoes cleavage. While this approach operationally simple, it requires complex …
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Newly Designed HNO Triggered Prodrugs
Nitric oxide (NO) is an important species in many biological processes. The one-electron reduced and protonated derivative of NO, HNO has also been determined to play important biological roles. Because of HNO’s high reactivity, its detection has been difficult and many methods including …
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Carbon Monoxide Prodrugs for Targeted Cancer Therapy
… prompting the development of novel CO-releasing prodrugs. This thesis presents the design and development of radical-activated, metal-free CO-prodrugs. The prodrugs are designed to address delivery limitations and avoid metal-associated toxicity. These tertiary aldehyde-based prodrugs are stable …
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Synthesis of Novel CYP1 Activated Heterocyclic Anticancer Prodrugs
… novel target for the development of anti-cancer prodrugs, which would remain non-toxic until undergoing metabolism to toxic species by CYP1 enzymes over-expressed at tumour sites. The chalcones have been shown to exhibit effective anti-cancer prodrug activity, but are labile to photoisomerisation …
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Glycan polymeric prodrugs against pulmonary intracellular alveolar infections
… multivalent glycopolymer prodrug systems. Prodrugs are inactive forms of the drug, but when administered undergo hydrolysis to release the pharmacologically active drug. We hypothesized that engineering mannose glycopolymer prodrugs to target the macrophage mannose receptor on alveolar …
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Fluoromethyl ketone prodrugs: Potential new insecticides towards Anopheles gambiae
… of these compounds were prepared as potential prodrugs. These structures identified trifluoromethyl ketone oxime 3-2d as a potent toxin against both wild-type (G3-strain) and a multiply resistant (Akron) strain of An. gambiae. This compound is within 3-fold of the toxicity of propoxur to wild …
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BIOACTIVATION OF NATURAL DIETARY PRODRUGS BY SPECIFIC CYTOCHROME P450 ENZYMES
… The enzymes are used to activate nontoxic prodrugs with latent activity. Thus, the combination of tumour specific CYPs as ‘rescue enzymes’ with a suitable substrate provides a platform to develop selective anticancer prodrugs. This thesis describes the bioactivation of natural prodrugs by …
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Stereoisomeric Prodrugs to Improve Ocular And Oral Absorption of Prednisolone
… of this project is to develop stereoisomeric prodrugs such as Lvaline- D-valine-prednisolone (LDP) and D-valine-L-valine-prednisolone (DLP) to improve ocular and oral absorption of prednisolone. These prodrugs have been examined for their interaction with various influx and efflux transporters …
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Synthesis and pharmacological evaluation of novel anti-tumour prodrugs. Synthesis and pharmacological investigations into novel MMP-activated peptide-based prodrugs of methotrexate as potential cancer therapeutics
… in various ways, not least via the design of prodrugs. The concept of tumour protease, and specifically matrix metalloproteinase (MMP), activated prodrugs was the focus of the work described in this thesis. This concept relies upon attachment of an MMP-sensitive peptide sequence to a specific …
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Synthesis of D-alanyl-D-alanine dipeptide isosteres and cephalosporin prodrugs
Resistance to vancomycin by enterococci is of great clinical importance. Vancomycin inhibits bacterial growth by binding to terminal D-alanyl-D-alanine linkages in the growing peptidoglycan cell wall. Synthesis of dipeptide isosteres which may be incorporated into the growing cell wall is …
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New applications of Imidazotetrazinone prodrugs. Synthesis and mechanistic investigation of novel imidazotetrazinones as prodrugs of aziridines and as traceless carriers for drug delivery to the central nervous system.
New imidazotetrazinones have been synthesised that possess features in their structures to release aziridinium ions upon ring opening. Unstable 2-aminoethylisocyanates were required in this preparation, which were synthesized with BOC-protection of the amino group to counteract the reactivity of …
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SYNTHESIS AND SCREENING OF PI3K INHIBITOR PRODRUGS FOR TREATMENT OF PROSTATE CANCER
Prostate cancer is the most common non-skin cancer in American men. At the current time, there is no effective treatment for men with metastatic prostate cancer. Androgen ablation is the most successful systemic treatment for prostate cancer. However, the cancer eventually recurs as …
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Great Expectations: Phosph(On)Ate Prodrugs In Drug Design—Opportunities and Limitations
… been successfully overcome through the use of prodrugs. When attached to the phosph(on)ate moiety, prodrugs mask the negative charge and easily enable cell permeability. Upon cellular entry, the promoieties are enzymatically or environmentally cleaved to unveil the active pharmacophore. A …
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Synthesis and MAO activity of a series of benzimidazolyl and indazolyl prodrugs
… activity of several indazolyl and benzimidazolyl prodrugs that are designed to release an enzyme inhibitor in the affected brain area. These studies have provided information regarding the nucleophilic aromatic substitutions of the ambident nucleophiles under consideration. We have also discovered …
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Pharmacological investigations into matrix metalloproteinase-activated anti-tumour prodrugs. In vitro metabolic and pharmacological investigations into a series of colchicine-based peptide prodrugs activated by tumour-expressed matrix metalloproteinases
… used agents. The stability of MMP-activated prodrugs in normal tissue or organs is a significant challenge for their success in the clinic. In an in vitro study, the stability of twenty six prodrugs was studied in mouse liver, kidney, lung and tumour homogenates using HPLC and LC/MS. Selected …
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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 of this …
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Mechanism of Action and Gold Nanoparticle Delivery of Pt(IV) Prodrugs of Cisplatin
… effects of platinum(IV) complexes, considered prodrugs for cisplatin, are believed to be due to biological reduction of Pt(IV) to Pt(II), with the reduction products binding to DNA and other cellular targets. In this work we used pBR322 DNA to capture the products of reduction of oxoplatin, …
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Maleinimid-funktionalisierte wasserlösliche Derivate klinisch etablierter Zytostatika – albuminbindende Prodrugs für eine verbesserte Chemotherapie
… umsetzen. <br>Albuminbindende Prodrugs des Zytostatikums CPT zeigen eine gegenüber CPT bis zu 27fach gesteigerte Wasserlöslichkeit und binden schnell und selektiv an Humanserumalbumin (HSA), wie durch HPLC-Experimente belegt werden konnte. In einer abschließend durchgeführten …
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