Abstract
As part of the ongoing research for more effective antimalarial drug, Fe (III) complex of mefloquine hydrochloride (antimalarial drug) was synthesized using template method. Mefloquine was tentatively found to have coordinated through the hydroxyl and the two nitrogen atoms in the quinoline and piperidine in the structure, respectively. Characterization has been done on the basis of analytical, conductance, atomic absorption, magnetic measurement, electronic and Infra-red spectrometry. From analytical data, the stoichiometry of the complex has been found to be 1:1. Infra-red spectral data also suggest that the ligand (mefloquine) behaves as a tridentate ligand with N:N:O donor sequence towards the metal ion. On the basis of the above physico-chemical data it is proposed that the complex is assigned octahedral geometry. The antimicrobial activities of mefloquine metal complex exhibited greater inhibition than the parent ligand. The ligand and metal complex were screened for their toxicological activities at the dose of 6.66 mg/kg body weight twice daily for seven days on the alkaline phosphatase (ALP), alanine aminotranferase (ALT) and aspartate aminotransferase (AST) activities of rat serum, liver and kidney. Overall, it was revealed that both mefloquine and its metal complex might show mild toxicity particularly on the liver and kidney. Key words: Fe(III) complex, synthesis, anti-malarial drug, antimicrobial, toxicology.
Highlights
Malaria is a parasitic disease that has brought misery and death to many parts of the world
The ligand and metal complex were screened for their toxicological activities at the dose of 6.66 mg/kg body weight twice daily for seven days on the alkaline phosphatase (ALP), alanine aminotranferase (ALT) and aspartate aminotransferase (AST) activities of rat serum, liver and kidney
Mefloquine hydrochloride is (±)-erythro-α-(2-piperidyl)-2,8-bis(trifluoromethyl) -4-quinoline methanol, are known for their antimalarial activity
Summary
Malaria is a parasitic disease that has brought misery and death to many parts of the world. Various studies have been carried out on complexation of some common antimalarial drugs with metals (Obaleye et al, 1997). The basic aim of the studies is to find molecules that would be more effective therapeutic substitutes for available antimalarial drugs that the malaria parasites had developed resistance against (Obaleye et al, 1999). Mefloquine hydrochloride (ligand employed in this study) is (±)-erythro-α-(2-piperidyl)-2,8-bis(trifluoromethyl) -4-quinoline methanol, are known for their antimalarial activity. Mefloquine is a white or slightly yellow, crystalline powder, very soluble in water, freely soluble in methanol and alcohol. It melts at about 260°C, with decomposition. Since the ligand (mefloquine) consists of potential binding sites such as oxygen and two nitrogen atoms, this work set out to study out the coordination tendencies, characterization after complexing with metal and the biological activities of mefloquine hydrochloride
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