Malaria is a parasitic infection that resulted in millions of cases and almost 900,000 deaths in the world in 2009. There are treatments for malaria, but many have begun to lose potency as the parasites gain resistance. Janet’s goal for the summer was to synthesize additional analogs of a lead compound from a chemical screen for antimalarials, in order to improve its solubility and potency.
Janet and her mentors worked to develop a viable synthesis route for the core scaffold of this lead chemical compound, and used TLC, LCMS, ISCO, and proton NMR to purify and confirm the products of each step of the reaction. Commercially available analogs of the lead compound were also purchased, and tested for potency and solubility. Preliminary data of potency and solubility showed that electron withdrawing groups resulted in a loss of potency. With a viable synthesis route for the production of the core scaffold of this compound, many more analogs may be synthesized in the future, to further improve potency and solubility of this potential antimalarial.
Janet, a senior at Medford High School, synthesized chemical compounds that are promising inhibitors of the malaria parasite, which is rapidly acquiring resistance against current treatments.