Investigação do perfil farmacológico antibacteriano e antifúngico de novos ditiocarbamatos de alguns metais representativos e de transição

Abstract

Due to resistance of some microorganisms new drugs have been investigated looking for high selectivity and low toxicity. In this work it was investigated the synthesis, characterization and the biocide activity of dithiocarbamate ligands and of their complexes. Two kind of dithiocarbamates have been used (i) the first set was prepared from alquilethanolamines (R = -CH3 (A), -CH2CH3 (B), -CH2CH2CH3 (C) and -CH2CH2OH (D)) and the second one (ii) was derived from atenolol. Complexes of Bi(III) and Ga(III) have been prepared using the route (i) and (ii) rendered complexes of Bi(III), Co(II), Ni(II), Pt(II) and Zn(II). Ligands and complexes have been fully characterization using infrared, 1H, 13C NMR, elemental analysis, melting point and X-ray diffraction for [Bi{S2CN(R)CH2CH2OH}3] {R = -CH2CH2CH3}. Then, the antifungal and antibacterial activity of all compounds have been screened in terms of agar diffusion tests and the minimal inhibitory concentration (MIC/mmol L-1), using Staphylococcus aureus (ATCC 25921), Escherechia coli (ATCC 11229), Candida albicans (ATCC 10231) and Candida tropicalis (Squibb 750). The toxicity and the biologic selectivity of the complexes were evaluated by measuring the cellular viability using methylene and acrydine-orange experiments. The higher toxicity was observed for ZnADTC, in view of the number of necrotic cells, and the other derivatives are less toxic. The mitosis inhibition observed by complexes [Ga{S2CN(R)CH2CH2OH}3] {R = -CH3 and -CH2CH3} suggests an antitumor activity, however some further tests are necessary