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Organic Synthesis and Testing of Novel Compounds in Search of New Broad-Spectrum Antibacterial and Liver-Stage Antimalarial Drugs

  • Author(s): Gentry, Jmelle Joseph
  • Advisor(s): Siegel, Dionicio R
  • et al.
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Abstract

The war between humans and microbes is as old as our existence. Humans have created antibiotics since 1928 to protect ourselves however, bacteria have consistently evolved to develop resistance to these antibiotics. While bacteria are a major threat to humans, they are not the only microbes that pose a threat to our survival. Protozoan parasites of the Plasmodium species cause 219 million cases of malaria annually. Malaria continues to threaten nearly half of the world’s population. In this research, two types of compounds were synthesized. Compound 7, a molecule that is similar in structure to tricyclic gyrase inhibitors was synthesized in hopes of discovering the next broad-spectrum, dual action antibiotic. Minimum Inhibitory Concentration assays were used to test the compound against six antibiotic-resistant bacterial strains. The tricyclic gyrase inhibitors were difficult to synthesized due to the benzylic properties of the starting materials. Compound 7 was synthesized but did not demonstrate antibiotic activity when tested against the bacteria. Other dicyclic amines were synthesized in hopes of creating a compound that selectively target Plasmodium parasites in the asexual liver stage over the asexual blood stages because it is less likely for the parasite to develop resistance. MP 28 and MP 51 were successfully synthesized. The Half Maximal Inhibitory Concentration (IC50) values will be used to determine the efficacy of the compounds against the Plasmodium falciparum parasite. The synthesized antimalarial compounds have not yet been tested.

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This item is under embargo until June 24, 2021.