Identification of small-molecule inhibitors of Trypansoma cruzi replication

  • Bioorg Med Chem Lett. 2011 Dec 1;21(23):7197-200. doi: 10.1016/j.bmcl.2011.09.057.
Andrew R Germain  1 ,  Leigh C Carmody ,  Chris Dockendorff ,  Cristina Galan-Rodriguez ,  Ana Rodriguez ,  Stephen Johnston ,  Joshua A Bittker ,  Lawrence MacPherson ,  Sivaraman Dandapani ,  Michelle Palmer ,  Stuart L Schreiber ,  Benito Munoz
Affiliations
  • 1. Chemical Biology Platform and Probe Development Center, Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA.
PMID: 22018462 DOI: 10.1016/j.bmcl.2011.09.057
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).

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