RESUMEN
A novel bismuth(III) complex with 2-amino-3-carbomethoxy-4,5,6,7-tetrahydrobenzo[b]thiophene (ACTT) as a ligand have been synthesized. The novel complex was characterized on the basis of its IR, NMR, elemental analysis and MS spectral data. It was found that the ligand behaves as a monodentate chelating agent and bonds to the metal ion through the nitrogen atom of the amino group to form the [BiIII(ACTT)6]Cl3 complex. The new complex compound displayed significant antimicrobial activity (MIC = 8-32 µg/mL) against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Shigella flexneri, Candida albicans, Candida tropicalis and Cryptococcus neoformans.
Asunto(s)
Antibacterianos/farmacología , Antifúngicos/farmacología , Complejos de Coordinación/farmacología , Tiofenos/farmacología , Antibacterianos/síntesis química , Antifúngicos/síntesis química , Bacterias/efectos de los fármacos , Bismuto/química , Candida albicans/efectos de los fármacos , Candida tropicalis/efectos de los fármacos , Complejos de Coordinación/síntesis química , Ligandos , Pruebas de Sensibilidad Microbiana , Tiofenos/síntesis químicaRESUMEN
The increasing recognition and importance of fungal infections, the difficulties encountered in their treatment and the increase in resistance to antifungal agents have stimulated the search for therapeutic alternatives. The objective of this study was to evaluate the antifungal activities of three substituted 2-aminothiophenes (1, 2 and 3) against some fungal species. The synthesis of substituted 2-aminothiophenes was carried out through the most versatile synthetic method developed by Gewald et al. The antifungal activity was performed against yeast, dermatophytes and Aspergillus species using the broth microdilution method. The effect of these aminothiophenes was examined on the protein content and profile. Compound 2 was the most active (MIC varying from 2.00 to 128 µg ml(-1) ). All the three substituted 2-aminothiophenes had a relatively important dose-dependent effect on Microsporum gypseum protein profile and content. These compounds affected the structure and dye fixation of macroconidia of this fungus. The overall results indicate that the tested substituted 2-aminothiophenes can be used as precursors for new antifungal drugs development.
