Background: Antimicrobial resistance is one of the most pressing health issues of our time. The increase in the number of antibiotic-resistant bacteria allied to the lack of new antibiotics has contributed to the current crisis. It has been predicted that if this situation is not dealt with, we will be facing 10 million deaths due to multidrug resistant infections per year by 2050, surpassing cancer-related deaths.
View Article and Find Full Text PDFSeveral metal-based carbon monoxide-releasing molecules (CORMs) are active CO donors with established antibacterial activity. Among them, CORM conjugates with azole antibiotics of type [Mn(CO)(2,2'-bipyridyl)(azole)] display important synergies against several microbes. We carried out a structure-activity relationship study based upon the lead structure of [Mn(CO)(Bpy)(Ctz)] by producing clotrimazole (Ctz) conjugates with varying metal and ligands.
View Article and Find Full Text PDFA series of new -[Mn(L)(CO)Br] complexes where L is a bidentate chelating ligand containing mixed mesoionic triazolylidene-pyridine (MIC^py, ), triazolylidene-triazole (MIC^trz, ), and triazole-pyridine (trz^py, ) ligands have been prepared and fully characterized, including the single crystal X-ray diffraction studies of and . The abilities of - and complex -[Mn(MIC^MIC)(CO)Br] () to catalyze the electroreduction of CO has been assessed for the first time. It was found that all complexes displayed a current increase under CO atmosphere, being and the most active complexes.
View Article and Find Full Text PDFThe antiproliferative activity of [Mn(CO)(N^N)Br] (N^N = phendione 1, bipy 3) and of the two newly synthesized Mn complexes [Mn(CO)(acridine)(phendione)]OTf (2) and [Mn(CO)(di-triazole)Br] (4) has been evaluated by MTS against three tumor cell lines A2780 (ovarian carcinoma), HCT116 (colorectal carcinoma), HCT116doxR (colorectal carcinoma resistant to doxorubicin), and in human dermal fibroblasts. The antiproliferative assay showed a dose-dependent effect higher in complex 1 and 2 with a selectivity toward ovarian carcinoma cell line 21 times higher than in human fibroblasts. Exposure of A2780 cells to IC concentrations of complex 1 and 2 led to an increase of reactive oxygen species that led to the activation of cell death mechanisms, namely via intrinsic apoptosis for 2 and autophagy and extrinsic apoptosis for 1.
View Article and Find Full Text PDFA new series of half-sandwich ruthenium(II) compounds [(η-arene)Ru(L)Cl][CFSO] bearing 1,2,3-triazole ligands (arene = -cymene, L = (); arene = -cymene, L = (); arene = benzene, L = (); arene = benzene, (); = 2-[1-(-tolyl)-1-1,2,3-triazol-4-yl]pyridine and = 1,1'-di--tolyl-1,1'-4,4'-bi(1,2,3-triazole) have been synthesized and fully characterized by H and C NMR and IR spectroscopy, mass spectrometry, and elemental analysis. The molecular structures of , , and have been determined by single-crystal X-ray diffraction. The cytotoxic activity of - was evaluated using the MTS assay against human tumor cells, namely ovarian carcinoma (A2780), colorectal carcinoma (HCT116), and colorectal carcinoma resistant to doxorubicin (HCT116dox), and against normal primary fibroblasts.
View Article and Find Full Text PDFNew manganese complexes bearing di-triazolylidene (di-trz) ligands are described. Depending on the wingtip substituents of the triazolylidene ligand and the synthetic procedure, two different ligand coordination modes were observed, i.e, bridging and chelating.
View Article and Find Full Text PDFNew unsymmetrical aminosquarylium cyanine dyes were synthesized and their potential as photosensitizers evaluated. New dyes, derived from benzothiazole and quinoline, were prepared by nucleophilic substitution of the corresponding O-methylated, the key intermediate that was obtained by methylation with CFSOCH of the related zwitterionic unsymmetrical dye, with ammonia and methylamine, respectively. All three news dyes herein described displayed intense and narrow bands in the Vis/NIR region (693-714nm) and their singlet oxygen formation quantum yields ranged from 0.
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