title: Screening and Identification of Inhibitors of Trypanosoma brucei Cathepsin L with Antitrypanosomal Activity.
abstract: Current treatment options for human African trypanosomiasis (HAT) are ineffective, and they have several well-known clinical limitations. In our continued efforts to identify chemotypes that can be developed into clinically useful drugs, we screened a targeted compound library against the major cathepsin L (rhodesain) in T. brucei. We report the antirhodesain activity and antitrypanosomal activity of the compounds in this letter. The identified compounds can serve as starting points for structure- and/or phenotype-based lead optimization strategy against Trypanosoma brucei.
authors.affiliation: Department of Chemistry and Biochemistry, Jackson State University, 1325 John R. Lynch Street, Jackson, MS, 39217, USA.
authors.forename: Tierra
authors.initials: T
authors.lastname: Jefferson
authors.affiliation: Department of Chemistry and Biochemistry, Jackson State University, 1325 John R. Lynch Street, Jackson, MS, 39217, USA.
authors.forename: Danielle
authors.initials: D
authors.lastname: McShan
authors.affiliation: Department of Chemistry and Biochemistry, Jackson State University, 1325 John R. Lynch Street, Jackson, MS, 39217, USA.
authors.forename: Jasmine
authors.initials: J
authors.lastname: Warfield
authors.affiliation: Department of Chemistry and Biochemistry, Jackson State University, 1325 John R. Lynch Street, Jackson, MS, 39217, USA.
authors.forename: Ifedayo Victor
authors.initials: IV
authors.lastname: Ogungbe
mesh_terms: D056668:Cathepsin L / Q000037:antagonists & inhibitors*; D056945:Hep G2 Cells; D006801:Humans; D014344:Trypanocidal Agents / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000201:enzymology*
chemical_list: D014344:Trypanocidal Agents; D056668:Cathepsin L
keywords: antitrypanosomal; dianiline; malaria box; rhodesain; trypanosomes