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1.
Molecules ; 19(4): 5402-20, 2014 Apr 24.
Artículo en Inglés | MEDLINE | ID: mdl-24879585

RESUMEN

The in vitro antifungal activity of nine dirutheniumpentadithiocarbamate complexes C1-C9 was investigated and assessed for its activity against four different fungal species with clinical interest and related to invasive fungal infections (IFIs), such as Candida spp. [C. albicans (two clinical isolates), C. glabrata, C. krusei, C. parapsolisis, C. tropicalis, C.dubliniensis (six clinical isolates)], Paracoccidioides brasiliensis (seven clinical isolates), Cryptococcus neoformans and Sporothrix schenckii. All synthesized complexes C1-C9 and also the free ligands L1-L9 were submitted to in vitro tests against those fungi and the results are very promising, since some of the obtained MIC (minimal inhibitory concentration) values were very low (from 10-6 mol mL-1 to 10-8 mol mL-1) against all investigated clinically relevant fungal pathogens, except for C. glabrata, that the MIC values are close to the ones obtained for fluconazole, the standard antifungal agent tested. Preliminary structure-activity relations (SAR) might be suggested and a strong influence from steric and lipophilic parameters in the antifungal activity can be noticed. Cytotoxicity assays (IC50) showed that the complexes are not as toxic (IC50 values are much higher-30 to 200 fold-than MIC values). These ruthenium complexes are very promising lead compounds for novel antifungal drug development, especially in IFIs, one of most harmful emerging infection diseases (EIDs).


Asunto(s)
Antifúngicos/farmacología , Candida/efectos de los fármacos , Complejos de Coordinación/farmacología , Animales , Antifúngicos/toxicidad , Candida/fisiología , Línea Celular , Supervivencia Celular/efectos de los fármacos , Complejos de Coordinación/toxicidad , Cricetinae , Cryptococcus neoformans/efectos de los fármacos , Cryptococcus neoformans/fisiología , Humanos , Concentración 50 Inhibidora , Pruebas de Sensibilidad Microbiana , Rutenio/química , Sporothrix/efectos de los fármacos , Sporothrix/fisiología , Tiocarbamatos/química
2.
Chem Biol Drug Des ; 78(5): 810-5, 2011 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-21756287

RESUMEN

Aldimines are aldehyde-derived compounds that contain a C=N group. Besides its broad industrial applications, this class of non-naturally occurring compounds are found to possess antibacterial, antifungal, antimalarial, antiproliferative, anti-inflammatory, antiviral, and antipyretic properties. Based on this, six aryl aldimines were synthesized from the condensation of aromatic amines with benzaldehydes. The antifungal activities of synthesized compounds were evaluated against nineteen fungal strains that included Candida and Aspergillus species, Cryptococcus neoformans. The aryl aldimines 2-(benzylideneamino)phenol (3) and 4-(benzylideneamino)phenol (8) were the most active compounds against the fungi studied. Compounds 3 and 8 efficiently inhibited the metabolism of C. neoformans mature biofilm.


Asunto(s)
Antifúngicos/síntesis química , Antifúngicos/farmacología , Compuestos de Bencilideno/química , Candida/efectos de los fármacos , Cryptococcus neoformans/efectos de los fármacos , Fenoles/farmacología , Antifúngicos/química , Biopelículas/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Fenoles/síntesis química , Fenoles/química
3.
Mycoses ; 54(5): e323-9, 2011 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-20557461

RESUMEN

The in vitro antifungal activity of ruthenium dithiocarbamate compounds (1-5) was investigated and assessed for its activity against seven different species of Aspergillus (Aspergillus clavatus, Aspergillus flavus, Aspergillus fumigatus, Aspergillus niger, Aspergillus nomius, Aspergillus tamarii and Aspergillus terreus). Analysis of in vitro susceptibility was performed using broth microdilution assay following the Clinical and Laboratory Standards Institute guidelines for filamentous fungi. The cytotoxicity was evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Aspergillus clavatus and A. fumigatus were more susceptible species for complexes 1 and 2. Other complexes showed excellent minimum inhibitory concentration (4-64 µg ml(-1)) against most microorganisms. Complexes 1 and 2 are respectively 180- and 95-fold more active than the corresponding free ligands against A. clavatus and the complex 5 is 46-fold more active than free ligand against A. niger. Aspergillus niger was more susceptible to the action of the complexes 1 and 5 (16 µg ml(-1)). A low cytotoxic activity (IC(50) > 10(-6) mol l(-1) ) on normal mammalian cells (BHK-21) to the evaluated complexes was measured. Ruthenium complexes are promising antifungal agents against the development of novel effective drug against different species of Aspergillus; however, for A. nomius and A. terreus, they were not active in the highest concentration tested.


Asunto(s)
Aspergillus/efectos de los fármacos , Compuestos de Rutenio/química , Compuestos de Rutenio/farmacología , Tiocarbamatos/química , Tiocarbamatos/farmacología , Animales , Línea Celular , Supervivencia Celular/efectos de los fármacos , Cricetinae , Pruebas de Sensibilidad Microbiana , Compuestos de Rutenio/toxicidad , Tiocarbamatos/toxicidad
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