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Bioorg Med Chem Lett DOI:10.1016/j.bmcl.2011.09.057

Identification of small-molecule inhibitors of Trypansoma cruzi replication.

Publication TypeJournal Article
Year of Publication2011
AuthorsGermain, AR, Carmody, LC, Dockendorff, C, Galan-Rodriguez, C, Rodriguez, A, Johnston, S, Bittker, JA, MacPherson, L, Dandapani, S, Palmer, M, Schreiber, SL, Munoz, B
JournalBioorg Med Chem Lett
Volume21
Issue23
Pages7197-200
Date Published2011 Dec 01
ISSN1464-3405
KeywordsInhibitory Concentration 50, Molecular Structure, Small Molecule Libraries, Structure-Activity Relationship, Trypanocidal Agents, Trypanosoma cruzi
Abstract

We report the outcome of a high-throughput small-molecule screen to identify novel, nontoxic, inhibitors of Trypansoma cruzi, as potential starting points for therapeutics to treat for both the acute and chronic stages of Chagas disease. Two compounds were identified that displayed nanomolar inhibition of T. cruzi and an absence of activity against host cells at the highest tested dose. These compounds have been registered with NIH Molecular Libraries Program (probes ML157 and ML158).

DOI10.1016/j.bmcl.2011.09.057
Pubmed

http://www.ncbi.nlm.nih.gov/pubmed/22018462?dopt=Abstract

Alternate JournalBioorg. Med. Chem. Lett.
PubMed ID22018462
Grant List1 U54 HG005032-1 / HG / NHGRI NIH HHS / United States
/ / Howard Hughes Medical Institute / United States