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    OXAZOLIDINONES AS A PRIVILEGED SCAFFOLD AND PRELIMINARY EVALUATION

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    Genre
    Thesis/Dissertation
    Date
    2022
    Author
    Day, Brian M.
    Advisor
    Canney, Daniel J.
    Blass, Benjamin E.
    Committee member
    Nagar, Swati
    Department
    Pharmaceutical Sciences
    Subject
    Pharmaceutical sciences
    5-HT7
    Antifungal
    Ketoconazole analogs
    Kinase
    Oxazolidinone
    Privileged scaffold
    Permanent link to this record
    http://hdl.handle.net/20.500.12613/8317
    
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    DOI
    http://dx.doi.org/10.34944/dspace/8288
    Abstract
    Drug discovery contains many strategies, one of which is the privileged scaffold strategy. This strategy incorporates a similar molecular framework within a collection of drug-like compounds in order to target various receptors. These scaffolds are useful to drug discovery scientists since they assist in developing libraries as well as demonstrating selectivity to a target. Oxazolidinones are 5-membered heterocyclic compound containing an oxygen, a nitrogen, and a carbonyl within the ring system. In this present study, the oxazolidinone structure was utilized as a privileged scaffold to target serotonin receptor 7 (5-HT7), mutated BRAF kinase (BRAFV6000E), Bruton’s tyrosine kinase (BTK), and Cyclin-dependent protein kinase 4 and 6 (CDK4/6). Aryl piperazines and piperidines were integrated as another privileged scaffold to support the selectivity towards 5-HT7, while aminopyrimidines were employed to increase binding against the kinases. The 5-HT7 oxazolidinone series was successfully synthesized and analyzed against 5-HT7; however, the three kinase oxazolidinone series were not successfully synthesized.Candidemia is the most common bloodstream infection in the U.S. and is associated with high patient mortality rates. Due to prolonged and/or repeated clinical use of current antifungal agents, drug-resistant fungi have become an emerging problem. There is a need for new antifungals to assist in overcoming drug resistant fungi. In the second project outlined in this work, a series of ketoconazole analogs were designed and successfully synthesized. The ketoconazole analogs exhibited antifungal activity; however, no clear trends were observed in this series. Overall, the series exhibited less CYP3A4 inhibition than the parent compound, ketoconazole.
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