Organic Chemicals Commons^™

Second Generation Phenyloxadiazolyl Methyl Sulfones For Thiol-Specific Bioconjugations, Guillaume Dewaele-Le Roi

Dissertations, Theses, and Capstone Projects

The role of antibody-based molecular agents for diagnosis and therapy of cancer has expanded significantly over the past decades. However, most of these constructs are synthesized using traditional bioconjugation methods based on the random ligations between the molecular cargo and lysine residues within the protein. These non-specific approaches can create poorly defined conjugates with suboptimal immunoreactivity and in vivo performance while Site-specific approaches to antibody bioconjugation based on ligations between maleimides and free cysteine residues have long stood as attractive alternatives. Yet the inherent instability of the thiol-maleimide linkage has fueled the search for new, more stable thiol-reactive prosthetic groups. …

Designing And Synthesizing A Warhead-Fragment Inhibitory Ligand For Ivyp1 Through Fragment-Based Drug Discovery, Samuel Moore

Symposium of Student Scholars

Fragment-based drug discovery (FBDD) is a powerful tool for developing anticancer and antimicrobial agents. Within this, magnetic resonance spectroscopy (NMR) provides a comprehensive qualitative and quantitative approach to screening and validating weak and robust binders with targeted proteins, making NMR among the most attractive strategies in FBDD. Inhibitor of vertebrate lysozyme (Ivyp1) of P. aeruginosa serves as an excellent target because of its active cellular location and implications in clinical prognosis for cystic fibrosis and immunocompromised patients. This study uses current NMR and biophysical techniques to develop a covalent, fragment-linked warhead inhibitor for Ivyp1 through synthetic methods, warhead linking, and …

Exploring Alternative Treatment Options For A Patient With Heavy Menstrual Bleeding And Mistrust Of The Healthcare System, Rachel A. O'Dell

Clinical Research in Practice: The Journal of Team Hippocrates

A clinical decision report using:

Tinelli A, Gustapane S, D’Oria O, Licchelli M, Panese G. Nutraceuticals in fibroid management after ulipristal acetate administration: An observational study on patients’ compliance. International Journal of Gynecology and Obstetrics; 2022;156(1):133-138. https://doi.org/10.1002/ijgo.13692

for a patient with chronic, symptomatic anemia with menorrhagia and uterine fibroid.

Biomedical Applications Of Protein Films And Polymeric Nanomaterials, Sanjana Gopalakrishnan

Doctoral Dissertations

Biomaterials are widely applied for the diagnosis and treatment of numerous diseases. In addition to fulfilling specific biological functions, biomaterials must also be non-toxic, biocompatible, and sterilizable to be regarded as safe-for-use. Polymers are excellent candidates for fabricating functional biomaterials due to their wide availability and varied properties and may be natural or synthetic. Polymer precursors are fabricated into coatings, foams, scaffolds, gels, composites, and nanomaterials for several biomedical applications. This dissertation focuses on two types of polymeric biomaterials – protein-based materials and synthetic polymeric nanoparticles. Proteins are biopolymers that naturally occur with a variety of structural and functional properties. …

The Kinetics And Cellular Imaging Of Multi-Color Fluorescent And Chemiluminescent Compounds, Bo Li

Chemistry Theses and Dissertations

A three-dimensional display is a useful method which can provide spatially accurate representations of high-resolution images with a 360^° view. Therefore, it has potential to be applied widely in the medical area, entertainment industry and for military applications. According to the first-generation 3D digital light photoactivatable dye display (3D Light PAD), N-phenyl spirolactam rhodamine B was used as photoactivatable compound that could be switched from non-fluorescent to fluorescent using ultraviolet light. However, the detailed mechanism, how other rhodamine derivatives would perform in 3D Light PAD, and what other factors in this system could improve the imaging quality remained unclear. …

Effect Of Nicotine On Immune Suppression And Prostate Cancer Pathogenesis, Sirin Saranyutanon

Theses and Dissertations

Tobacco or cigarette smoking is the leading cause of several diseases, including cancer, in the United States and worldwide. Epidemiological data provide strong evidence for an association of nicotine with prostate cancer risk and recurrence, but experimental data is largely lacking. Nicotine is an addictive ingredient of tobacco products and other alternatives, however, its role in prostate tumor biology has not been explored. Further, while a role of smoking in immunosuppression has been demonstrated, the effect of nicotine on immune function is largely unknown. We hypothesized that nicotine suppresses immune function by promoting alternative polarization of macrophages and promotes prostate …

Synthesis Of Triaminopyrimidine Derivatives For Inhibition Of Inflammatory Caspases, Marianna C. Haddad, Caitlin Karver

DePaul Discoveries

Caspases are cysteine-dependent aspartic proteases whose functions are connected to different mechanisms of cell death and inflammation. As caspase-1 plays a significant role in the immune response, its activity has been of interest as a target for inhibitor development as its inhibition will reduce the levels of pro-inflammatory cytokines in inflammatory diseases, thus minimizing the symptoms that arise and serving as a possible therapeutic approach. Prior work discovered a family of potent inhibitors of caspase-1 with a common triaminopyrimidine scaffold. To further explore structure-activity relationship profiles of potential inhibitors of caspase-1, two different syntheses were attempted to create two new …

Diisopinocampheylborane Trifluoromethanesulfonate-Mediated Aldol Reactions Using An Aldehyde And An Amide, Camille Parker

Honors Theses

Aldol reactions are one of the most powerful reactions in organic chemistry because of the formation of new carbon-carbon bonds. A downside of aldol reactions is that they generate a mix of stereoisomers, therefore a lot of work has gone into developing methods that selectively favor a certain stereoisomer. We report an enatio and diastereoselective diisopinocampheylborane trifluoromethanesulfonate ((Ipc)₂BOTf) mediated aldol reaction with an amide and an aldehyde. Traditionally, (Ipc)₂BOTf-mediated reactions were not applied to amides, except with the use of strong bases. Here we developed a (Ipc)₂BOTf aldol reaction of amides using mild bases …

Synthesis, Characterization, And Bioactivity Of 3-Substituted Coumarins As An Undergraduate Project, Karsen King, Nicholas Campbell, Ronald Okoth, Wathsala Medawala

Georgia Journal of Science

Coumarins are an important class of phytochemicals, a chemical defense presumed to be secreted by plants. More recently, Coumarins have gathered popularity for their basis in anti-cancer agents. This paper dives into the organic synthesis of two 3-substituted coumarins from o-vanillin using the Knoevenagel condensation reaction. The 3-substituted coumarin were characterized using melting point analysis, ¹H-NMR, and UV-Vis spectroscopy. In addition, the anticancer activity of synthesized 3-substituted coumarin compounds were assayed against topoisomeraseIIα, which is the target enzyme of FDA approved anti-cancer drug etoposide since it is an active enzyme in cancer cell replication. The demonstrated procedures can be …

Synthesis Of A Functionalized Trans-Cyclooctene (Tco) For Selective Protein Isolation After Bioorthogonal Labeling With Tetrazine, Thaddeus Lawrence Puzdrakiewicz, Dillon P. Mcbee, Joshua A. Baccile

Chancellor’s Honors Program Projects

No abstract provided.

Drug-Facilitated Sexual Assault At The University Of Arkansas, Barrett Weidman

Chemical Engineering Undergraduate Honors Theses

This work was written to fulfill two main purposes. First, to help survivors of Drug-Facilitated Sexual Assault (DFSA) process their experience by compiling the toxicological, pharmacological, and distribution of the three most used date-rape drugs. Second, to gauge the knowledge and interest of University of Arkansas students regarding drug impairments, sexual assault education, and bystander intervention training. A survey was conducted for the latter and revealed that 91.6% of students believe the University’s existing sexual assault prevention education and bystander intervention training have room for improvement. Also, 37.1% of students who have received this education report that the programming does …

Bis(Tryptophan) Amphiphiles: Design, Synthesis And Efficacy As Antimicrobial Agents, Michael Mckeever

Dissertations

Amphiphiles play important roles in nature. These molecules contain both hydrophilic and hydrophobic regions, leading to some astonishing properties. The lipid bilayer of the cell membrane is a fascinating organization of amphiphilic phospholipids. Natural and synthetic amphiphiles, such as antimicrobial peptides, interact with the cell membrane. Such interactions can impact transport of molecules across the cell membrane, disrupting cell functions. In this work, a library of tryptophan-containing amphiphiles was synthesized and their antimicrobial properties were explored.

First, a library of bis(tryptophan) amphiphiles was synthesized. Preparation included a coupling reaction of a diamine with tryptophan residues, via their carboxy-termini, at …

A Quantitative Analysis Of The Efficacy Of Various Essential Oils Against The Sars Cov-2 Virus, Elizabeth Wagstaff, Chandrelyn Kraczek, Jack Brandon Lopez

Annual Research Symposium

A poster presentation and abstract for the Roseman Symposium. The project focuses on testing 3 essential oil blends and two disinfectants containing an essential oil blend against SARS CoV-2 in response to the COVID-19 pandemic. The project procedure involves plaque assays, disinfection, and neutralization techniques.

Use Of Steroids In Covid-19 Patients: What Is Known?, Syed Muhammad Mustahsan, Marzia Tahir, Emaduddin Siddiqui

Department of Emergency Medicine

COVID-19 pandemic has exaggerated the role of steroids in the standard of care despite minimum direct evidence of their efficacy in COVID-19 patients and their well-known adverse effects. The literature abounds on the side effects of steroids affecting different organ systems of the body. COVID-19 patients, who are on long-term steroids, are more susceptible to their adverse effects. We, herein, briefly review the potential uses and the adverse effects of steroids on different organ systems of the body. Key Words: Steroids, COVID-19, Adverse effects.

Synthesis Of Selenotryptophan For Protein Elucidation, James P. Reiselman

Belmont University Research Symposium (BURS)

Through complex intermolecular and intramolecular forces, proteins conformationally change to form complex 3-d geometry that carries out biochemical processes and mapping their structures is becoming a field of interest in the biological community. Techniques for modeling protein’s structure typically follow the path of X-ray crystallography, which has an intrinsic phase problem that can make reading the electron density map they produce very difficult. This can be mitigated by appending a heavy-atom containing amino acid analogue into a crystal sample of the protein being studied. A selenium containing tryptophan analogue will be synthesized to be appended into proteins as a chemical …

Synthesis Of Trifluoromethyl Ketones By (Diethylamino) Sulfur Trifluoride (Dast)-Mediated Nucleophilic Trifluoromethylation Of Benzoic Acids, Michael A. Vescio

Honors College Theses

Within the past few decades, the presence of fluorine containing

organic molecules has increased significantly. Many of the

current industrial production methods are not cost-effective,

practical, or inherently safe. This work describes a new methodology

for the synthesis of trifluoromethyl ketones. Our new method involves

the use of benzoic acid and trifluoromethyl trimethylsilane (TMSCF₃) as starting

materials along with diethylamino sulfur trifluoride (DAST) as a reagent

to obtain moderate to good yields of expected products in a short

reaction times.

The Benefits Of Astaxanthin To Improve Pain Relief In Patients With Painful Diabetic Neuropathy: An Open-Label, Randomized Controlled Trial, Rizaldy Taslim Pinzon, Mary Rose Angelina Budi Harsana

Pharmaceutical Sciences and Research

Treatment of diabetic neuropathy is still carried out by providing symptomatic therapy, which only improves ± 50% of the total symptoms felt by patients, but does not tackle the underlying causes of the disease. Astaxanthin is a potent antioxidant, anti-inflammatory, and anti-diabetic carotenoid that could be an additional treatment option. We aimed to measure the effectiveness of administering astaxanthin as an additional therapy to improve the impact of pain and discomfort experienced daily by diabetes mellitus patients with painful diabetic neuropathy. We conducted a randomized experimental study with an open label design of 36 patients who had been diagnosed with …

Design And Synthesis Of Small Molecular Probes For Cns And Kidney Disorders, Swagat H. Sharma

Theses & Dissertations

The G protein regulated inwardly rectifying potassium channels (GIRK) are a family of inwardly rectifying potassium channels and are key effectors in signaling pathways. GIRK 1/2 channel subunit, predominantly found in the brain, is involved pathophysiology of various neurological disorders including, but not limited to, epilepsy, anxiety, Parkinson's, pain, reward, and addiction. Previously, our laboratory had identified a series of urea containing molecules as GIRK1/2 preferring activators. Unfortunately, the urea series suffers from significant PK liabilities (solubility, brain penetration and high clearance). The chapter 1 of the dissertation describes our efforts in developing three new series of activators with improved …

Continuous Liquid-Liquid Extraction Of Lomustine Synthesis, Devna Grover

The Journal of Purdue Undergraduate Research

No abstract provided.

Polymer-Based Strategies For Therapeutic Delivery To Bacterial Biofilms, Cheng-Hsuan Li

Doctoral Dissertations

Bacterial infections are emerging threat to public health. Antibiotics once provided front-line treatments to bacterial infections; however, bacteria adapted to resist antibiotics through drug resistance mechanisms and biofilm formation. In this dissertation, I describe polymer-based strategies for therapeutic delivery as treatments of bacterial biofilm infections. Initially, I developed a functional polymer for delivering hydrophobic carvacrol (the primary constituent of oregano oil) to the bacterial biofilms. This strategy incorporates a cross-linking strategy to fabricate a robust yet biodegradable nanoemulsion, improving antimicrobial activity of carvacrol and overcoming antimicrobial resistance development. Next, I demonstrated that this functional polymer-based emulsion platform provides a general …