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PREPARATION AND EVALUATION OF PEPTIDYL ACYLOXYMETHYL KETONES FOR CATHEPSIN B IMAGINGEdem, Patricia 10 1900 (has links)
<p>This thesis describes the initial steps towards the use of dipeptidyl acyloxymethyl ketones as a platform to develop molecular imaging (MI) probes for cancer. Initially the synthesis of an AOMK was performed following a literature procedure which resulted in an epimerized product. This issue was addressed by optimizing an alternative method yielding all intermediates in yields similar or better to those reported in the literature (final product yield of 67%). An AOMK derivative that can be used to evaluate target expression levels was synthesized by linking a fluorescent dye to the ε-amine group of lysine in accordance to a literature procedure describing the synthesis of an optical imaging probe in 24% yield. A second generation derivative AOMK was prepared by linking 4-fluoro-benzoic acid to the same amino group yielding a model of a PET MI probe.</p> <p>An endpoint colorimetric assay was developed and optimized to test cathepsin B inhibitors. Due to the fact that the AOMKs exhibit time-dependent inhibition these assay conditions did not prove to be adequate for the assessment of the cathepsin B binding. Steps toward developing a continuous assay that would be better suited for these compounds were achieved. Factors such as the relationship between the formation of the assay product vs enzyme concentration and determination of the Michelis-Menten constant (K<sub>m</sub> = 390 ± 30 nM) were established. These parameters can be used to determine the optimal enzyme and substrate concentration that should be used to test the AOMK based probes.</p> / Master of Science (MSc)
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Evaluation of the antioxidant and anti-inflammatory activities of synthetic 2-styrylchromonesGomes, Ana Maria de Carvalhais Mendes 22 December 2009 (has links)
Doutoramento em Química Farmacêutica / PhD Degree - Pharmaceutical Chemistry
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Pharmaceutical salt formation guided by phase diagrams /Lam, Ka Wing. January 2009 (has links)
Includes bibliographical references (p. 107-121).
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Design and synthesis of bioactive small molecules and high-throughput identification of enantiomeric excess.Onaran, Mehmet B. January 2008 (has links)
Thesis (Ph.D.)--Brown University, 2008. / Vita. Advisor : Christopher T. Seto. Includes bibliographical references.
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The effects of humidity and lactose grade on pharmaceutical inhalation formulationsWatling, Christopher Peter January 2009 (has links)
No description available.
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New tools for flow chemistry and the machine assisted synthesis of pharmaceuticalsDeadman, Benjamin Jade January 2013 (has links)
No description available.
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Sythesis of mazindol derivatives as potential irreversible antagonists of cocaine and other stimulantsSepcic, Kelly Hall 08 1900 (has links)
No description available.
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The total synthesis of 3-hydroxy-17-deaza-17-thiamorphinan, 3-hydroxy-17-deaza-17-thiaisomorphinan, and 3-methoxy-17-deaza-17-thia-[delta] ̳9, ̳10 - hasubanan /Camicioli, J. Richard M. (Joseph Richard Marc) January 1983 (has links)
No description available.
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The action of drugs on potassium-evoked release of acetylcholine from rat hippocampal prisms with special reference to tacrine and classical cholinesterase inhibitorsAmerasinghe, Nirosha Devika January 1995 (has links)
No description available.
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Bioanalysis of ibuprofen enantiomers : application to pharmacokinetic studies in young and elderly volunteersTan, Soo Choon January 1996 (has links)
No description available.
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