title: Ro 15-0216: a nitroimidazole compound active in vitro against human and animal pathogenic African trypanosomes.
abstract: In vitro systems for the continuous cultivation of Trypanosoma brucei brucei, T. b. gambiense, T. b. rhodesiense, T. congolense and T. vivax were used to determine the antitrypanosomal activity of the 2-substituted nitroimidazole Ro 15-0216. For all trypanosome species, the concentration which inhibited parasite growth by 50% (IC50 value) was established: 0.0957 microgram ml-1 (T. b. brucei TC221), 0.1327 microgram ml-1 (T. b. gambiense STIB 754-A), 0.0450 microgram ml-1 (T. b. rhodesiense STIB 704-BABA), 0.0896 microgram ml-1 (T. congolense ILNat 3.1) and 0.0109 microgram ml-1 (T. vivax ILRAD 1392). The IC50 value of its major metabolite Ro 19-9638 was 0.0341 microgram ml-1 (T. b. rhodesiense STIB 704-BABA). Furthermore, minimum exposure times required to render T. b. brucei non-infective for mice as well as preventing their growth in vitro have been established to be three, four, six and ten hours at drug concentrations of 30, 10, 3 and 1 microgram ml-1, respectively.
authors.affiliation: International Laboratory for Research on Animal Diseases, Nairobi, Kenya.
authors.forename: N K
authors.initials: NK
authors.lastname: Borowy
authors.forename: R T
authors.initials: RT
authors.lastname: Nelson
authors.forename: H
authors.initials: H
authors.lastname: Hirumi
authors.forename: R
authors.initials: R
authors.lastname: Brun
authors.forename: H K
authors.initials: HK
authors.lastname: Waithaka
authors.forename: D
authors.initials: D
authors.lastname: Schwartz
authors.forename: A
authors.initials: A
authors.lastname: Polak
mesh_terms: D000083:Acetanilides / Q000494:pharmacology*; D000818:Animals; D009593:Nitroimidazoles / Q000494:pharmacology*; D014344:Trypanocidal Agents; D014345:Trypanosoma / Q000187:drug effects* / Q000472:pathogenicity; D014346:Trypanosoma brucei brucei / Q000187:drug effects; D014347:Trypanosoma brucei gambiense / Q000187:drug effects; D014348:Trypanosoma congolense / Q000187:drug effects
chemical_list: D000083:Acetanilides; D009593:Nitroimidazoles; D014344:Trypanocidal Agents; C056694:Ro 19-9638; C054646:Ro 15-0216