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Full-Text Articles in Chemicals and Drugs

Design And Synthesis Of Small Molecule Drugs For Cns Disorders, Kirsten T. Tolentino Aug 2023

Design And Synthesis Of Small Molecule Drugs For Cns Disorders, Kirsten T. Tolentino

Theses & Dissertations

Dopamine (DA) is an important neurotransmitter for the regulation and long-term function of the central nervous system (CNS). DA binds to Dopamine Receptors (DR) to stimulate or inhibit adenyl cyclase production to further elicit a pharmacological response. DRs were cloned, and it was determined that there are two families separated by their function and five total subtypes distinguished by their amino acid structure. The Dopamine 4 receptor (D4R) is the second least studied subtype but has high expression in the frontal cortex, amygdala, hippocampus, hypothalamus, globus pallidus, substantia nigra pars reticula, and thalamus. Dopamine signaling and transmission, especially in the …


Diisopinocampheylborane Trifluoromethanesulfonate-Mediated Aldol Reactions Using An Aldehyde And An Amide, Camille Parker Jun 2022

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 …


Base-Labile Protecting Groups For Stepwise Peg Synthesis, Logan D. Mikesell Jan 2021

Base-Labile Protecting Groups For Stepwise Peg Synthesis, Logan D. Mikesell

Dissertations, Master's Theses and Master's Reports

Stepwise synthesis of monodisperse polyethylene glycols (PEGs) and their derivatives usually involves using an acid-labile protecting group such as DMTr and coupling two PEG moieties together under the basic Williamson ether formation conditions. Using this approach, each elongation of PEG is achieved in three steps – deprotection, deprotonation, and coupling – in two pots. Here, we report a more convenient approach for PEG synthesis featuring the use of a base-labile protecting group such as the phenethyl group. Using this approach, each elongation of PEG can be achieved in only two steps – deprotection and coupling – in one pot. The …


Synthesis And Characterization Of Pamam-Fatty Acid “Janus-Type” Dendritic Hybrids For Biomedical Applications, Abigail Grace Barker May 2020

Synthesis And Characterization Of Pamam-Fatty Acid “Janus-Type” Dendritic Hybrids For Biomedical Applications, Abigail Grace Barker

Honors Theses

Janus dendrimers are amphiphilic macromolecules that have shown promising potential in the biomedical field. Due to their unique structure and properties, these branched block copolymers have the ability to self-assemble into bioinspired spherical nanoaggregates. Because they possess a hydrophobic and hydrophilic moiety, these aggregates show potential as drug delivery systems that can transport both hydrophobic and hydrophilic drugs. However, many of the proposed dendrimer systems suffer from certain weaknesses that hinder their practical usage as clinical treatment options. Some of these shortcomings include specificity, solubility, size, surface charge, and mechanical properties. To combat these problems, we synthesized and characterized a …