Drug discovery for human African trypanosomiasis: Identification of novel scaffolds by the newly developed HTS SYBR Green assay for Trypanosoma brucei

by Faria J, Moraes CB, Song R, Pascoalino BS, Lee N, Siqueira-Neto JL, Cruz DJM,  Parkinson T, Ioset JR, Cordeiro-da-Silva A, Freitas-Junior LH. Journal of Biomolecular Screening 2014, doi:10.1177/1087057114556236.

Summary: High-throughput screening (HTS) of small-molecule libraries in whole-cell assays is one of the most frequently used approaches in drug discovery for infectious diseases. To aid in drug discovery efforts for HAT, a new assay (the SYBR Green assay) was developed for T. brucei in a 384-well format. This semi-automated assay is cost- and time-effective, robust, and reproducible. When compared to the existing resazurin assay by screening a selective library of 4000 compounds it showed superior performance in terms of assay time, sensitivity, simplicity, and reproducibility, and resulted in a higher hit confirmation rate. Compounds with the most potent antitrypanosomal activity were selected from both screens and several new scaffolds as antitrypanosomal agents identified which show promise as new starting points for drug discovery for HAT.

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