In vitro antiplasmodial activity and cytotoxicity of newly synthesized N-alkyl and N-benzyl-1,10-phenanthroline derivatives.

A previous study showed that the 1,10-phenanthroline skeleton was active in vitro against chloroquine-resistant and sensitive strains of Plasmodium falciparum. Based on this skeleton, 8 derivatives of N-alkyl and N-benzyl-1,10-phenanthrolines have been synthesized. This study was conducted to evaluate the in vitro antiplasmodial activity and cytotoxicity of these compounds. The in vitro antiplasmodial activity was tested on two strains of P. falciparum, FCR-3 chloroquine-resistant and D10 chloroquine-sensitive strains, while their cytotoxicity was tested on the Vero cell line. The parasite and cell growth were estimated by hypoxantine-[2,8-3H] uptake after 24- and 72-hour incubation with each compound tested. The control parasite or cell free from any compounds was referred to as having 100% growth. For this radioactive method, the IC50 value showing concentration inhibiting 50% of the parasite growth was determined by probit analysis. The results showed that the highest antiplasmodial activity was observed with (1)-N-benzyl-1,10-phenanthrolinium iodide with the IC50 0.18-0.45 microM, and the IC50 of the compound on Vero cells ranged from 2,582.30 to 7,057.71 microM. The cytotoxic/ antiplasmodial ratio indicates that this compound has high selectivity (10,993 +/- 330.79-38,965 +/- 6,888.27).

characterization of chemical and electrochemical synthesis of some metal chelates derived from ethyl benzoylacetate hydrazide

Coordination compounds of some transition metal ions with the hydrazide derivative of ethyl benzoyl acetate were synthesized by both chemical and electrochemical techniques. Their structures were elucidated by elemental analysis, molar conductance, magnetic susceptibility [at 25 degree] and spectral [IR, UV-vis, esr] studies. The IR spectra showed that the ligand reacted mostly in the enol form except for the complex derived from hydrated Cu [II] sulfate. The thermal stability of the complexes was investigated by differential thermal analysis [DTA]

Preparation and characterization of cadmium [II] keto-stabilized phosphonium or sulfonium complexes

Two new sets of cadmium complexes were prepared from the reaction of phosphonium or sulfonium salts with cadmium chloride. The complexes have the general formulae [CdL Cl2] and [CdL2] Cl2 and were characterized by elemental analysis and conductance measurements. The IR spectra of the complexes showed that the CO group of the phosphonium or sulfonium salts coordinates to the central Cd [II] ion. Electronic spectra used to study the spatial distribution of the ligands around the central cadmium [II] ion