Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors

ACS Med Chem Lett. 2020 Jan 10;11(3):249-257. doi: 10.1021/acsmedchemlett.9b00453. eCollection 2020 Mar 12.


Utilizing a target repurposing and parasite-hopping approach, we tested a previously reported library of compounds that were active against Trypanosoma brucei, plus 31 new compounds, against a variety of protozoan parasites including Trypanosoma cruzi, Leishmania major, Leishmania donovani, and Plasmodium falciparum. This led to the discovery of several compounds with submicromolar activities and improved physicochemical properties that are early leads toward the development of chemotherapeutic agents against kinetoplastid diseases and malaria.