Resumen de Open Synthesis Network Research in an Undergraduate Laboratory: Development of Benzoxazole Amide Derivatives against Leishmania Parasite
Scott C. Faville, Kes Harris Hamdscomb, Owain Harker, Stephanie Mattison, Hajie Tamorite, Joshua Bristowe, Daniel Daly, Raissa Ege, Haoyuan He, Julian Jones, Abby McCorkindale, Kerry Mei, Ashleigh Monson, Lana Moree, Finley Perkovic, Georgia Rickerby, Jack Robinson, Felix Rudkin, Luke Whibley, Rebecca Worthington, Courtney Ennis, Sara de la Harpe, Thomasin Brind, Andrew Hopkins, Kaleb Winefield, Sarah Hendrickx, Guy Caljon, Benjamin Perry, Andrea J. Vernall
An undergraduate laboratory was developed as part of the Drugs for Neglected Diseases initiative’s Open Synthesis Network. This activity aimed to develop new compounds efficacious against visceral leishmaniasis. Students successfully synthesized, purified, and characterized ten different benzoxazole amides that were sent for biological testing against several protozoan parasites. Although all the benzoxazole amides had poor activity against L. donovani, several (2, 4, and 9) showed moderate activity against T. cruzi, T. b. rhodesiense, and T. b. brucei paired with low cell cytotoxicity. This drug discovery laboratory activity made a measurable contribution to neglected tropical disease research and was an engaging and research-orientated experience for undergraduate students. Implementation of drug discovery 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.
