In the current study, we report new 3,5-disubtitutedpyrazole derivativeswhich are nitrogen and oxygen containing compounds with antiplasmodial activity. Evidence from existing literature shows potential antiplasmodial activity of new compounds containing nitrogen and sulphur. 10 The compounds were synthesized and evaluated for their antiplasmodial activity. They were also screened for their in vitro antimalarial activity against chloroquine-resistant strain of P.falciparum. The compounds shows more potentactivity thanpositivecontroland exhibited reasonable in silico drug-likeness and pharmacokinetic properties. 12
Materials and Methods
ReagentsAll reagents used were of analytical grade, only few were of reagent grade and they were all used without further purification.Phenylacetylchloride (98%), 3,5pyrazoledicarboxylic acid mono hydrate (97%), and the metal salts were products of Sigma Aldrich.Other reagents like chloroform (98%), ethanol (98%), and tetrahydro furan (THF) were obtained from Fluka. General Procedure for the Synthesis of 5-((2phenylacetoxy) carbonyl)-1H-pyrazole-3-carboxylic acid The ligand, 5-((2-phenylacetoxy) carbonyl)-1H-pyrazole-3-carboxylic acid was prepared by adopting methods reported in literature. 13,14 To equal mixture of chloroform and ethanol (50 mL), 2.612 g (5 mmol) of 3,5-Pyrazole dicarboxylic acid was added followed by 2.0 mL of phenylacetyl chloride under reflux for 2 h. The solution was left to stand for 2 weeks. A white crystal was obtained by filtration (Scheme 1).
Synthesis of the ComplexesThe Ce(III), Pr(III) and Nd(III) complexes of the ligand were prepared according to the method described by Heinosuke (1967). 15 Generally, the ligand was reacted separately with the metal salts using mole ratio 2:1 under reflux for 2 h and the products formed were filtered and stored in the desiccator for further use.