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Our lab has been looking at new compounds from which to develop potential antimalarial drugs. Much of our efforts go into chemically modifying classes of molecules known to bind to enzyme active sites, but that haven't been developed for use against malaria. As one example, we have been able to modify tetrahydroquinolonic (THIQ) amides to obtain several new compounds with high activity in several assays against Plasmodium falciparum, the malaria causing organism. These same compounds already are showing excellent metabolic and availability properties in vitro and in animals. One THIQ (SJ733) is currently in phase 1b human clinical trials, and has been funded for Phase 2. This research is currently the subject of a five year NIH grant proposal.
The Aresty Scholar will be asked to learn the techniques of organic synthesis on scales from several milligrams to several grams. New compounds will have to be purified and characterized spectroscopically; their biological evaluation will be done off-site by our collaborators. The student will also learn aspects of modern medicinal chemistry, as well as process chemistry, and will develop knowledge of organic and biochemical mechanism and the planning of synthetic routes. The student will interact with research group members, off-site collaborators, and other malaria and medicinal chemistry experts, and will have the opportunity to publish and patent the results of the research. In the few years, three papers have been published with Aresty-supported co-authors.
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