Cu-catalyzed click reaction in synthesis of eugenol derivatives as potent antimalarial agents.

Eugenol(), a terpenoid found in Ocimum, has various biological activities. The present study aims at extraction, isolation of the plant secondary metabolite eugenol (), it's derivatisation and structure identification as bioactive molecules. Synthesis and antiplasmodial activity ( and ), of a series of fourteen novel eugenol-based 1,2,3-triazole derivatives was done in the present study. Derivatives - showed good antimalarial activity against the strain NF. Derivative , IC at 2.85 µM was found to be several times better than its precursor (106.82 µM) whereas the derivative showed three fold better activity than compound , . The structure-activity relationship of the synthesised compounds indicated that the presence of triazole ring in eugenol analogues is responsible for their good activity. Compound , was further evaluated for antimalarial activity which showed about 79% parasitemia suppression. It is the first report on antimalarial activity of triazole eugenol derivatives.