Open Synthesis Network Research in an Undergraduate Laboratory: Development of Benzoxazole Amide Derivatives against Leishmania Parasite

An undergraduate laboratory was developed as part of the Drugs for Neglected Diseasesinitiative's Open SynthesisNetwork. This activity aimed to develop new compoundsefficacious against visceral leishmaniasis. Students successfullysynthesized, purified, and characterized ten different benzoxazoleamides that were sent for biological testing against severalprotozoan parasites. Although all the benzoxazole amides hadpoor activity againstL. donovani, several (2,4, and9) showedmoderate activity againstT. cruzi,T. b. rhodesiense, andT. b. bruceipaired with low cell cytotoxicity. This drug discovery laboratoryactivity made a measurable contribution to neglected tropicaldisease research and was an engaging and research-orientatedexperience for undergraduate students. Implementation of drugdiscovery laboratories across a range of student levels and backgrounds is highly achievable using existing laboratory equipment and a short investment in activity preparation and can be a sustainable course component