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Showing 1 to 20 of 34 for “"Medicinal Chemistry and Pharmaceutics"”.
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Islet Dysfunction In Diabetes
… failure of pancreatic beta cells to synthesize and secrete sufficient insulin to meet the metabolic demands and the inability of tissues [muscle, adipose and liver] to efficiently utilize the secreted insulin leading to an overall increase in blood glucose levels [hyperglycemia]. As indicated by …
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Design, Synthesis, Biological Evaluation And Molecular Modeling Studies Of Novel Multifunctional Neuroprotective Drugs For The Treatment Of Parkinson's Disease: An Effort Towards The Improvement Of In Vivo Efficacy And Modulation Of Alpha Synuclein Aggregation Property Of The Neuroprotective Parent
<p>DESIGN, SYNTHESIS, BIOLOGICAL EVALUATION AND MOLECULAR MODELING STUDIES OF NOVEL MULTIFUNCTIONAL NEUROPROTECTIVE DRUGS FOR THE TREATMENT OF PARKINSON'S DISEASE: AN EFFORT TOWARDS THE IMPROVEMENT OF IN VIVO EFFICACY AND MODULATION OF ALPHA SYNUCLEIN AGGREGATION PROPERTY OF THE NEUROPROTECTIVE …
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Mechanisms Of Cytokine-Induced Metabolic Dysfunction Of The Pancreatic Beta-Cell
… proinflammatory cytokines such as IL-1â, TNFá and INFã are secreted by infiltrated and activated T-cells and macrophages which ultimately damage the pancreatic â-cell. However, the signaling mechanisms involved in cytokine-induced damage are only partially understood. Phagocyte-like NADPH …
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Progress Towards Development Of Multifunctional, Dopamine D2/d3 Receptor Agonists As Symptomatic And Disease-Modifying Therapeutic Agents For Parkinson's Disease
… dopamine in the nigrostriatal pathway and ensuing loss of motor function. Common symptoms of PD include resting tremor, muscular rigidity, bradykinesia (slowness and decreased amplitude of movement), along with postural instability and cognitive psychiatric complications. PD affects 1% …
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Multifunctional bioreducible nanoparticles for gene therapy
… different types of therapeutic nucleic acids, and ease of formulation. However, low transgene efficiency and lack of targeting ability remain major challenges. Bioreducible polyplexes (polyelectrolyte complexes of disulfide-containing polycations and nucleic acids) utilize the redox potential …
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The impact of stress history of deformable dry granules on the mechanical properties of tablets
<p>A mechanistic understanding of the relationship among the granule composition, individual granule property, downstream robust processing, and the final tablet attributes is critical for rational development of a quality tablet. However, in the dry granulation literature, milled granules that are …
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Investigation onto the Mechanism Behind the Hepatoprotective Effect of Cucurbitacin Compounds
… tumors if they are diagnosed early. Chemotherapy and radiation treatments are not usually effective. They are mainly used to shrink a large tumor, so the resection can be done successfully. Thus, despite great strides made in therapy regimens, most treatments are destined to eventually fail. …
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Mechanisms of regulation of islet function by nadph oxidase
… secretion (GSIS) involves a series of metabolic and cationic events, leading to translocation of insulin-laden secretory granules from a distal site toward the plasma membrane for fusion and release of insulin into circulation. Vesicular transport and fusion events are tightly regulated by …
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Assay procedures for dehydroepiandrosterone
<p>Dehydroepiandrosterone (DHEA) is a 17-ketosteroid which is produced by the adrenal cortex and is excreted in the urine as DHEAsulfate, In diseases of the adrenal cortex, such as adrenal carcinoma or adrenal hyperactivity, the level of DHEA-sulfate in the urine is increased. There are two …
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Small gtp-binding proteins in insulin secretion
… is characterized by defective insulin secretion and resistance to insulin. Understanding the molecular events leading to Glucose-stimulated insulin secretion [GSIS] might serve as therapeutic potential towards diabetes. GSIS involves interplay between small G-proteins and their regulatory …
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The Effect of 48 hr Glucose Administration on the Hepatic P-450 System
… The spectral binding of hexobarbital and methadone to hepatic microsomal P-450 was found to be significantly reduced following glucose administration. The changes in spectral binding were observed in the absence of any significant change in the microsomal P-450 content. The changes in …
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Design Of Functional Dendrimer Nanocarriers And Their Formulations In Propellant-Based Inhalers For Pulmonary Drug Delivery
… inhalers for pulmonary drug / gene delivery to and through the lungs. First challenge is to design biocompatible moieties for the steric stabilization of suspension formulations in HFO-based propellants. Using a combination of tools including ab initio calculation, molecular dynamics simulation …
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Investigation of the absorptive potential of polymeric nanoparticles across the lungs and their development for efficient systemic delivery following pulmonary administration
… area available for absorption, a thin epithelium and extensive vasculature to name a few. Accordingly, a vast number of small molecule drugs, peptides, and proteins have been used to investigate their translocation across the lungs with many of the tested candidates showing excellent …
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Submonomer Synthesis and Structure-activity Relationship Studies of Azapeptide Inhibitors of the Insulin Receptor Tyrosine Kinase
… structures responsible for high affinity and selective binding to a target receptor or enzyme in order to modulate its activity for therapeutic purpose. Moreover, azapeptides have been found to be stable in biological media thereby improving their therapeutic indices and pharmacokinetic …
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Development of a Pharmaceutical Tablet Authentication system using Spectroscopic Techniques in combination with Multivariate Chemometric Methods
… to customers) is not well monitored and suffers the highest rates of fraudulent activities. Also, the rise of product procurement from the internet increases the chance of American consumers' exposure to poor quality drugs. To combat this horrendous activity, surveillance of …
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Progress Towards Understanding Of Mechanisms Of Action Of Potent Multifunctional Disease Modifying Therapeutics For Parkinson's Disease & Investigating The Methamphetamine-Induced Striatal Microglia Activation.
<p>PROGRESS TOWARDS UNDERSTANDING OF MECHANISMS OF ACTION OF POTENT MULTIFUNCTIONAL DISEASE MODIFYING </p> <p>THERAPEUTICS FOR PARKINSON'S DISEASE.</p> <p>by</p> <p>MRUDANG MANOJKUMAR SHAH</p> <p>December 2013</p> <p>Advisor: Dr. Aloke Dutta</p> <p>Major: Pharmaceutical Sciences</p> <p>Degree: …
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Formulation Devlopment Of Mesoporous Silica Nanoparticles As An Injectable Delivery System
<p>Our long term goal is to develop a versatile and robust injectable carrier based on Mesoporous Silica Nanoparticles (MSN) for drug/drug combination therapies. The objective of my dissertation was to optimize surface functionality, particle shape and methods of colloidal stabilization of …
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The structural requirements of histone deacetylase (hdac) inhibitors: suberoylanilide hydroxamic acid (saha) analogues modified at c3, c6, and c7 positions enhance selectivity
… (SAHA, Vorinostat), have cleared clinical trials and emerged as anti-cancer drugs. However, SAHA inhibits all of the 11 metal ion-dependent HDAC proteins. Therefore, we synthesized several libraries of small molecule HDAC inhibitors based on SAHA to help understand the structural requirements of …
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Dual Delivery Systems Based On Polyamine Analog Benspm As Prodrug And Gene Delivery Vectors
<p>Combination drug and gene therapy shows promise in cancer treatment. However, the success of such strategy requires careful selection of the therapeutic agents, as well as development of efficient delivery vectors. BENSpm (N1, N11-bisethylnorspermine), a polyamine analogue targeting the …
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