Design, synthesis, and activation of prodrugs of the sulfonamide drug TAK-242 (Resatorvid) for localized immunosuppression.

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dc.contributor.advisorKane, Robert R.
dc.creatorKostyo, Jessica H., 1995-
dc.creator.orcid0000-0001-7004-2159
dc.date.accessioned2024-07-30T12:43:58Z
dc.date.available2024-07-30T12:43:58Z
dc.date.created2023-12
dc.date.issued2023-12
dc.date.submittedDecember 2023
dc.date.updated2024-07-30T12:43:58Z
dc.description.abstractThe success of organ and cellular transplants relies heavily on the use of immunosuppressive drugs to prevent the host immune system from attacking and rejecting the transplant. However, the systemic use of immunosuppressants can lead to undesired off-target effects. As such, methods to locally deliver potent drugs are highly sought after. This dissertation details the synthesis and characterization of two families of small molecule prodrugs designed to locally inhibit the immune system, with a focus on the delivery of the potent TLR4 antagonist TAK-242 (Resatorvid). Following successful synthesis and characterization, the activation and function of the prodrugs were investigated in an aqueous buffer. Both families of prodrugs demonstrated that the rate of drug release could be modulated by altering select components of the prodrug. The experiments performed on the final prodrugs successfully demonstrated the effectiveness of these prodrug strategies in vitro and have led to further consideration for in vivo application as well as inspired another possible generation of prodrug.
dc.format.mimetypeapplication/pdf
dc.identifier.uri
dc.identifier.urihttps://hdl.handle.net/2104/12875
dc.language.isoEnglish
dc.rights.accessrightsNo access – contact librarywebmaster@baylor.edu
dc.titleDesign, synthesis, and activation of prodrugs of the sulfonamide drug TAK-242 (Resatorvid) for localized immunosuppression.
dc.typeThesis
dc.type.materialtext
local.embargo.lift2025-12-01
local.embargo.terms2025-12-01
thesis.degree.departmentBaylor University. Dept. of Chemistry & Biochemistry.
thesis.degree.grantorBaylor University
thesis.degree.namePh.D.
thesis.degree.programChemistry
thesis.degree.schoolBaylor University

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