Identification of small-molecule inhibitors of Trypansoma cruzi replication

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 inhibit...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-12, Vol.21 (23), p.7197-7200
Hauptverfasser:	Germain, Andrew R., Carmody, Leigh C., Dockendorff, Chris, Galan-Rodriguez, Cristina, Rodriguez, Ana, Johnston, Stephen, Bittker, Joshua A., MacPherson, Lawrence, Dandapani, Sivaraman, Palmer, Michelle, Schreiber, Stuart L., Munoz, Benito
Format:	Artikel
Sprache:	eng
Schlagworte:	Antibiotics. Antiinfectious agents. Antiparasitic agents Antiparasitic agents Biological and medical sciences Chagas disease chemistry Inhibitory Concentration 50 Medical sciences Molecular Libraries Probe Production Center Network (MLPCN) Molecular Structure Pharmacology. Drug treatments Small Molecule Libraries - chemistry Small Molecule Libraries - pharmacology Structure-Activity Relationship therapeutics Trypanocidal Agents - chemical synthesis Trypanocidal Agents - chemistry Trypanocidal Agents - pharmacology Trypanosoma cruzi - drug effects Trypansoma cruzi
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Zusammenfassung:	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).
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.09.057