Dataset Information

Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors.

ABSTRACT: 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.

SUBMITTER: Singh B

PROVIDER: S-EPMC7073875 | biostudies-literature | 2020 Mar

REPOSITORIES: biostudies-literature

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Publications

Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors.

Singh Baljinder B Bernatchez Jean A JA McCall Laura-Isobel LI Calvet Claudia M CM Ackermann Jasmin J Souza Julia M JM Thomas Diane D Silva Everton M EM Bachovchin Kelly A KA Klug Dana M DM Jalani Hitesh B HB Bag Seema S Buskes Melissa J MJ Leed Susan E SE Roncal Norma E NE Penn Erica C EC Erath Jessey J Rodriguez Ana A Sciotti Richard J RJ Campbell Robert F RF McKerrow James J Siqueira-Neto Jair L JL Ferrins Lori L Pollastri Michael P MP

ACS medicinal chemistry letters 20200110 3

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 deve ...[more]

PMID: 32184953

Dataset Information

Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors.

Publications

Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors.

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