Curative effects of the antipiroplasms amicarbalide and imidocarb on Trypanosoma brucei infection in mice.
The babesicides imidocarb and amicarbalide, which have structural similarities to the antitrypanosomatid diamidines, proved active against Trypanosoma brucei mouse infections: both cured infections when doses were administered daily for 3 days 24 h post-inoculation (curative dose imidocarb, 10 mg/kg; amicarbalide, 25 mg/kg). Mice were considered cured after survival 30 days longer than untreated infected controls, with no trypanosomes present in blood or cerebrospinal fluid smears. Both agents also cured when administered 48 and 72 h after challenge with T. brucei and prolonged the lives of animals 94 h after challenge. The results are discussed in respect to the potential of these carbanilides and their precursors, the antitumor phthalanilides, as lead compounds in chemotherapy of mammalian trypanosomiases.
D000578:Amidines / Q000627:therapeutic use*; D000818:Animals; D002224:Carbanilides / Q000008:administration & dosage / Q000627:therapeutic use*; D055598:Chemical Phenomena; D002621:Chemistry; D004133:Diminazene / Q000627:therapeutic use; D005260:Female; D007095:Imidocarb / Q000008:administration & dosage / Q000627:therapeutic use*; D008297:Male; D051379:Mice; D010419:Pentamidine / Q000627:therapeutic use; D014344:Trypanocidal Agents / Q000008:administration & dosage / Q000627:therapeutic use*; D014346:Trypanosoma brucei brucei; D014353:Trypanosomiasis, African / Q000188:drug therapy*
D000578:Amidines; D002224:Carbanilides; D014344:Trypanocidal Agents; D010419:Pentamidine; D007095:Imidocarb; C001772:amicarbalide diisethionate; D004133:Diminazene