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 118 for “"Medicinal-Pharmaceutical Chemistry"”.
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Target Based Design And Synthesis of Heterocycles in the Potential Treatment of Cancer and Opportunistic Infection
<p>Dose limiting toxicity and development of multidrug resistance by the tumors are the major limitations of current cancer chemotherapy. Microtubule targeting agents (MTAs) are a structurally diverse set of compounds that disrupt microtubule dynamics and exert their anticancer effect. Among the …
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Protein and Water Modeling in Computer-Aided Drug Discovery
… and how it’s incorporated in drug projects in a pharmaceutical setting. I conclude the chapter by highlighting water modeling in biological systems as well as the importance of rotamer and protonation state assignment in protein modeling.</p> <p>In Chapter 2, I introduce our novel Rotamer and …
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One-Step Synthesis of Kanamycin Functionalized Gold Nanoparticles With Potent Antibacterial Activity Against Resistant Bacterial Strains
<p>On the verge of entering the post-antibiotic era, numerous efforts are in place to regain the losing potential of antibiotics which are proving ineffective against common bacterial infections. Engineered nanomaterials, especially gold nanoparticles (GNPs) capped with antibacterial agents are …
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Novel Modulation of Adenylyl Cyclase Type 2
<p>Adenylyl cyclase isoforms are distinctly modulated by G protein subunits and are therefore hypothesized to be uniquely regulated by proteins that influence G protein signaling. Activator of G protein signaling 3 (AGS3) is a G protein modulator that binds Gαi subunits in the GDP-bound state, …
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Thermochemistry and bond energies of acetohydrazide, amides and cyclic alkyl ethers
… and combustion reaction systems and atmospheric chemistry of small hydrocarbons. Thermochemical properties, [Delta]H _{f(298)}, S _{298} and Cp (T) (10K
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Synthesis towards synthetic adenosine receptor
Adenosine is a biologically important molecule as it acts as local modulator with cytoprotective function in the body. Adenosine accumulates in the extracellular space in response to metabolic stress and cell damage, and elevations in extracellular adenosine level are found in conditions like …
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Activity of Analogs of Anticancer Drugs on the Serine Protease Enzymes Subtilisin and Chymotrypsin
<p>The anticancer activity of several platinum compounds is due to the formation of complexes with DNA. We hypothesize that the size and shape of the platinum compounds would impact interaction with proteins, and these interactions may be partly responsible for the anticancer activity. Chymotrypsin …
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A Study on the Protein Interaction with Different Platinum Compounds
Since the discovery of anti-tumor activity of cisplatin in 1960, significant progress has been made in treating metastatic or advanced cancer with cisplatin and platinum compounds. Platinum compounds covalently bind to DNA and disrupt DNA function. They are also known to bind with amino acids like …
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Synthesis and Antifungal Evaluation of Barbiturate Saponins And Progress Towards Cysteinyl Metal Peptides
<p>Invasive fungal infections are a major threat to immune-compromised patients. There is a critical need to develop new antifungal agents because of increasing resistance to the common antifungal drugs.</p> <p>In the first part of this dissertation, methods for preparation of novel barbiturate …
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Monitoring Dissolution of Nonsteroidal Anti-Inflammatory Drugs Using Infrared Spectroscopy
<p>A comparison study was conducted to look at the formulation of three brands of naproxen sodium. These brands included Bayer Aleve ®, CVS All Day Pain Relief and Walgreens All Day Pain Relief. The active and inactive ingredients were the same yet the size and shape of the tablets differ among the …
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Synthesis of a Resveratrol Glycinate Derivative.
<p>Recently, the compound resveratrol has had media attention as an anti carcinogen. However, the bioavailability of resveratrol is low in the human system due to its hydrophobic nature. Therefore, it must be administered in high dosages to be effective. A plethora of derivatives have been …
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Synthesis and Biological Evaluation of Rigid Analogues of Methamphetamines
<p>A series of rigid azetidenyl-based methamphetamine analogs were synthesized from commercially available <em>N</em>-Boc-azetidinone. The benzylideneazetidine analogs were prepared via a Wittig olefination via the ylides generated from the corresponding triphenylphosphonium benzylhalide salts. The …
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Synthesis of Bulky and Polar Galactonoamidines for the Inhibition of the Human α-Galactosidase
… make them important drug targets for study in medicinal chemistry. The seminal work by Pauling and Wolfenden showed that enzymes bind to their substrate at the transition state with very strong affinity. Wolfenden estimated the dissociation constant to be around 10-22M. This encouraged the …
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Size Dependent Antimicrobial Properties of Sugar Encapsulated Gold Nanoparticles
… 60 nm, and 120 nm (± 5 nm) synthesized by green chemistry principles were investigated against both Gram-negative and Gram-positive bacteria. Studies were performed involving the effect of the dGNPs on the growth, morphology and the ultrastructural properties of bacteria. dGNPs were found to have …
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Syntheses of a Tin (IV) meso-Tetra(4-pyridyl) Porphyrin Dichloride-Tetrachlorobis (Bipy)2 Ruthenium (II) Complex and Studies of Photophysical Properties of 1-Nitropyrene
<p>Development of a photosensitizer that can work in both aerobic and anaerobic environments would increase the robustness of the cancer treatment known as photodynamic therapy. The development of a photosensitizer was first attempted by synthesizing a tin (IV) meso-tetra (4-pyridyl) porphyrin …
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DJ-1 AND ATP13A2: TWO PROTEINS INVOLVED IN PARKINSON’S DISEASE
<p>Parkinson's disease (PD) is the second most common neurodegenerative disorder after Alzheimer's disease, affecting approximately 0.3% of the total U.S. population, and its prevalence increases with age. Two neuropathological hallmarks of PD are the loss of dopaminergic neurons in the …
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Supercharging: An Investigation into the Effects of External Amino Acid Residue Charge on the Solubility and Internal Electric Character of Bound Ligands in a Heme-Binding de novo-Designed Protein
<p>De novo protein design offers many interesting prospects both as a means to better understand natural protein dynamics and as a potential resource in biomedical and industrial applications. In this work I describe the modification of a simple, well-characterized heme-binding protein by altering …
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