期刊
JOURNAL OF INORGANIC BIOCHEMISTRY
卷 89, 期 1-2, 页码 18-28出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/S0162-0134(01)00324-5
关键词
ternary copper(II) complexes; 1,10-phenanthroline; singly and dideprotonated salicylic acids; crystal structures; EPR spectroscopy; non-steroidal anti-inflammatory drugs; anti-convulsant properties
Two ternary Cu(II) complexes of 1,10-phenanthroline (phen) and singly (Hsal(-)) or dideprotonated (sal(2-)) salicylate ligands were synthesized, their X-ray crystal structure and electron paramagnetic resonance spectral characteristics determined, and evaluated for anti-convulsant activities in the maximal electroshock (MES) and Metrazol models of seizure and Rotorod toxicity. The X-ray crystal structure of [bis(1,10-phenanthroline)-mu-bis(salicylato-O,O')dicopper(II)] dihydrate, 1, {[Cu-2(II)(phen)(2)(sal)(2)].2[H2O]}, shows it to be binuclear. This dimer consists of two centrosymmetrically related pseudo-five coordinate Cu(II) atoms 3.242(2) Angstrom apart and bridged by two dideprotonated salicylate ligands. The X-ray crystal structure of [bis(1,10-phenanthroline)(salicylato)copper(II)][salicylate] monohydrate, 2. {[Cu-II(phen)(2)(Hsal)](+)[Hsal](-)[H2O]}, shows it to be mononuclear. This complex cation exhibits a highly irregular distorted square pyramidal geometry about the Cu(II) atom, (4+I+1*). Each salicylate is singly deprotonated and one of them is ligand bonded in an asymmetric chelating mode. EPR results for 2 indicate that in concentrated DMF solution phen remains bonded to copper but salicylate is likely monodentate in contrast to the situation for 1. However, in dilute DMF Solution, both I and 2 form the same species, which accounts for the similarity in anti-convulsant activity of the two compounds. Both I and 2 were found to be effective in preventing MES-induced seizures and ineffective in preventing Metrazol-induced seizures. Rotorod toxicity, consistent with central nervous system depression, paralleled the observed anti-convulsant activity. It is suggested that the observed anti-convulsant activity is consistent with central nervous system depression as a physiological mechanism in overcoming MES-induced seizures due to MES-induced brain inflammatory disease. (C) 2002 Elsevier Science Inc. All rights reserved.
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