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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 26 for “"Co-crystallization"”.
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Supramolecular derivatisation of bioactive molecules via co-crystallization and cyclodextrin inclusion complexation
… objective of this study was to modify the physicochemical properties of two common drugs via supramolecular derivatization. Sulfasalazine is a powerful anti-inflammatory drug and fluconazole has a strong antibacterial and antifungal activity. The common feature is their very low solubility in …
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The supramolecular derivatisation of pharmaceutically relevant compounds via co-crystallization and cyclodextrin inclusion complexation
… derivatisation of pharmaceutically relevant compounds via co-crystallization and cyclodextrin (CD) inclusion complexation was attempted in order to produce new solid forms of these compounds for potential pharmaceutical applications. The pharmaceutically relevant compounds investigated …
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Beneficiation of selected pesticides and an antihyperlipidemic agent via cyclodextrin complexation and co-crystallization
… molecules are limited by their undesirable physicochemical properties, such as poor aqueous solubility and low thermal stability. The agrochemicals methyl- 2,5-dichlorobenzoate (fungicide, DCB) and fenthion (insecticide), as well as the medicinal compound acipimox (lipid-lowering agent) were …
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TB-RBP protein : sitting at the crossroads of sex and disease
… of TB-RBP (Testis/Brain RNA binding protein) in complex with single stranded DNA. The secondary goal was to determine the crystal structure of TB-RBP in complex with Trax (translin associated factor X). Functions of TB-RBP is to suppresses translation of testicular mRNAs (Ex: protamines 1 and 2), …
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Co-crystal screening of poorly water-soluble active pharmaceutical ingredients. Application of hot stage microscopy on curcumin-nicotinamide system and construction of ternary phase diagram of fenbufen-nicotinamide-water co-crystal system.
… longa and has been reported to possess pharmacological activities. Unfortunately this compound suffers from poor bioavailability and rapid neutral-alkaline degradation. Co-crystal of curcumin is one option under exploration, motivated by the fact that a number of active pharmaceutical …
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The preparation and characterization of multi-component systems in drug pre-formulation
The supramolecular derivatisation, via co-crystallization and cyclodextrin (CD) inclusion of three active pharmaceutical ingredients (APIs), was attempted with the aim of generating new solid forms with potential pharmaceutical application. The APIs under investigation included allopurinol (used …
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Co-processing of drugs and co-crystal formers and its effect on pharmaceutical dosage-form performance. Co-crystallization of urea/ 2-methoxybenzamide, caffeine/ malonic acid, caffeine/ oxalic acid and theophylline/ malonic acid systems: Solid-state characterization including imaging, thermal, X-ray and Raman spectroscopic techniques with subsequent evaluation of tableting behaviour
… on the solid-state characterization of different co-crystal system as well as the effect of co-crystallization of these systems on pharmaceutical dosage form performance. Urea/ 2-MB, caffeine/ malonic acid, caffeine/ oxalic acid and theophylline/ malonic acid co-crystals were prepared using …
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High Performance Engineering Polymers: Design, Properties, and Performance
… polymerization techniques, a myriad of reaction conditions probed various polymer families including polysulfones, polyesters, polyimides and polyureas. Copolymers ranging from random to segmented sequences provided insight into the influence of segment length on physical properties. Melting …
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Single-crystal growth of organic semiconductors and organic electronic applications
… describes single crystal growth of organic semiconductors and their applications in organic electronics. In Chapter 2, a self-assembled monolayer of C60 derivatives with five carboxylic acids was employed to make C60 thin-film transistors. The highly-crystalline C60 monolayer enabled more …
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Crystallization studies of Pictet-Spenglerases
… source of therapeutic molecules. Due to the complexity of these molecules, biosynthesis of derivatives is an attractive way of obtaining molecules with potentially new or improved functionality. The rational design of mutants with altered/expanded substrate scope is an important step in …
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Structural investigation of 1,8-dinitro-4,5-dihydroxyanthraquinone and implications for docking as a small molecule inhibitor into the protease of West Nile virus
… its activity. However, the binding mechanism and conformation of the lead is unknown. The virtual screen that discovered this inhibitor showed it as having an unorthodox bend in the middle of the anthraquinone structure upon binding the protease. Upon further investigation, tautomerism and a bent …
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Towards Fluorinated Substrate Analogs and N-Acylated 2-Aminopyrimidine Inhibitors of Lipoxygenases
Cyclooxygenase (COX) and lipoxygenase (LOX) catalyze the rate-determining step in the production of arachidonic acid- derived signaling molecules (eicosanoids) within the body. COX has been extensively investigated, which has enabled the design of non-steroidal inflammatory drugs (NSAIDs) such as …
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Self-Consistency of the Lauritzen-Hoffman and Strobl Models of Polymer Crystallization Evaluated for Poly(ε-caprolactone) Fractions and Effect of Composition on the Phenomenon of Concurrent Crystallization in Polyethylene Blends
… were crystallized either isothermally or under constant cooling rate conditions suggested that the isothermal crystallization of the samples should be used for a proper evaluation of the molecular weight dependence of the observed melting temperature and degree of crystallinity in PCL. The …
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Development of large-scale colloidal crystallisation methods for the production of photonic crystals
Colloidal photonic crystals have potential light manipulation applications including; fabrication of efficient lasers and LEDs, improved optical sensors and interconnects, and improving photovoltaic efficiencies. One road-block of colloidal selfassembly is their inherent defects; however, they can …
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Predicting motif mimicry in viruses
… main pursuits in proteomics is to understand the complex network of protein-protein interactions (PPI) that underpin biological processes. Two major classes of PPI are domain-domain interactions (DDI) between globular proteins, and domain-motif interactions (DMI) between a globular domain and a …
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Engineering the angiotensin II type 1 receptor for structural studies
G protein-coupled receptors (GPCRs) are eukaryotic integral membrane proteins that perform transmembrane signal transduction. Due to their pivotal role in a wide range of essential physiological functions GPCRs represent a high proportion of all drug targets. High resolution X-ray structures of …
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Toward the structure and function of carbon-phosphorus lyase enzymes
… very stable carbon-phosphorus bond. Eshcherichia coli and many other strains of bacteria possess a multi-enzyme system called carbon-phosphorus (C-P) lyase that enables these organisms to cleave the C-P bond of organophosphonates when inorganic phosphate is scarce in the local environment. Genetic …
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Understanding the Atomic-Scale Mechanisms of the Human [alpha]4[beta]2 Nicotinic Acetylcholine Receptor
Nicotinic acetylcholine receptors are pentameric ligand-gated ion channels. These receptors are present in the central and peripheral nervous systems where they mediate fast synaptic transmission by allowing the flux of cations through the plasma membrane. The heteropentameric α4β2 subtype is the …
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DNA Binding Specificity of Mu Transcription Factor C and Crystallization of C : DNA Complex
… Mu is regulated by a transcriptional cascade consisting of early, middle and late transcription. The Mor protein is an activator of the middle promoter Pm and is encoded by the last gene of the early transcript. The C protein is an activator of the four late promoters Plys, PI, PP, and Pmom …
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Design, synthesis, and biological evaluation of Antimycobacterial agents from plant derived Betulinic acid, Oleanolic acid and their derivatives
… treatment of the disease are not effective for complete cure and in most cases, usually come with side effects, as a result of which new set of potent drugs are needed. In a quest to develop potent hit/drug leads for TB, betulinic acid (BA) and oleanolic acid (OA) were isolated respectively from …
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