ANTIFUNGAL NICKEL(II) COMPLEXES DERIVED FROM AMINO-SUGARS AGAINST PATHOGENIC YEAST, CANDIDA-ALBICANS

Nickel(II) complexes containing N-glycosides derived from D-glucosamin e (D-GlcN) and ethylenediamine (en) and trimethylenediamine (tn), [Ni( D-GlcN-en)(2)]Cl-2.H2O (1) (D-GlcN-en = 2-aminoethyl)amino}-2-amino-1, 2-dideoxy-D-glucose) and [Ni(D-GlcN-tn)(2)]Cl-2.4H(2)O (2) (D-GlcN-tn = 1-{(3-aminopropyl)amino}-2-amino-1, 2-dideoxy-D-glucose), are fairly stable in water at room temperature and showed effective antifungal a ctivity against pathogenic yeast, Candida albicans, with the MIC (mini mal concentration of inhibition) values of the complexes being 0.25 mM . The results obtained enzyme assays by using preparations of C. albic ans chitinase fraction suggested that the sugar complexes 1 and 2 play ed a role of novel chitinase (chitin-degradation enzyme) inhibitor, wh ere the modes of inhibition were competitive (K-i = 1.3 mM for 1, K-i = 1.8 mM for 2). The newly prepared nickel(II) complex 2 was character ized by elemental analysis, magnetic susceptibility, electronic absorp tion and circular dichroism spectroscopies, and an X-ray crystallograp hic analysis. (C) 1998 Elsevier Science Inc. All rights reserved.