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    CDRI-96/261-A novel Antileishmanial compound:

  • CDRI has discovered that compound 96-261 belonging to n-hydroxyalk-2-ene-1-one (together with its tautomeric form n-hydroxy-alkan-1,3-dione) display remarkable in vivo efficacy via oral route against L. donovani in hamsters. This is new use of a known compound. It is presumed that the compound selectively inhibits leishmanial dipeptidylcarboxypeptidase enzyme, a novel biochemical target for developing antileishmanial agent. This compound is cheap and active orally and can be synthesized in in a single step from readily available cheap starting material with good scale up capability. The compound display good solubility with good oral bioavailability. The ED50 for the drug has been found to be 41.50 mg/kg dose in hamster model. The initial pharmacokinetic parameters has revealed compound to be stable and traceable. Further PK evaluation to study its distribution in different tissues is underway. In the initial assay, the compound has found to be free of any hERG liability. The preliminary toxicity studies has revealed compound to be safe with large safety window (more than 50x X ED50).