Volume 12, Issue 4
  • ISSN: 0002-9637
  • E-ISSN: 1476-1645



The synthesis of CI-501 is described.

The drug was examined in mice and monkeys for potential value as a repository antimalarial substance. The dihydrotriazine moiety of CI-501 as the hydrochloride was tested in mice for background purposes. Activity was assessed on the basis of the period of protection against patent infections afforded by a parenteral dose prior to challenge with blood stages of or .

The duration of protection was directly related to the amount of CI-501 injected. Protection of mice ranged from 1 to 9 weeks with a subcutaneous dose of 50 to 660 mg/kg. In monkeys, protection ranged from 5 weeks to more than 94 weeks with an intramuscular or subcutaneous dose of 38 to 400 mg/kg. A gradual but strong therapeutic response in monkeys with patent infections was induced by 50 mg/kg intramuscularly. The doses used in mice and monkeys were well-tolerated, locally and systemically.

Corroborative evidence of a slow and sustained release of the active moiety from the injection site is cited from chemical tests, microbiological assays, and dialysis studies in rats.

The results of this first report on CI-501 encourage further study of it as a repository antimalarial drug.


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