RESUMEN
Our study presents innovative research dealing with the synthesis and biological evaluation of conjugates out of antimicrobial peptides (AMPs) and imidazolium cations that are derived from ionic liquids. AMPs are considered as promising alternatives to common antibiotics due to their different activity mechanisms. Antibacterial effects have also been described for ionic liquids bearing imidazolium cations . Besides single coupling of carboxy-functionalized imidazolium cations to the peptide N-terminal we also developed conjugates bearing multiple copies of imidazolium cations. The combination of both compounds resulted in synergistic effects that were most pronounced when more imidazolium cations were attached to the peptides. In addition, antibacterial activity even in drug-resistant bacterial strains could be observed. Moreover, the novel compounds showed good selectivity only against bacterial cells, an observation that was further proven by lipid interaction studies using giant unilamellar vesicles.
Asunto(s)
Antiinfecciosos/química , Antiinfecciosos/farmacología , Imidazoles/química , Péptidos/química , Farmacorresistencia Bacteriana/efectos de los fármacos , Eritrocitos , Humanos , Líquidos Iónicos/química , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Péptidos/síntesis química , Péptidos/farmacología , Sales (Química)/química , Técnicas de Síntesis en Fase Sólida , Relación Estructura-ActividadRESUMEN
Progress in homogeneous catalysis depends upon an understanding of the reaction mechanism; in asymmetric catalysis this entails an insight into the origins of enantioselectivity. Significant advances have been made in the area of alkene reduction catalyzed by rhodium or ruthenium complexes, which has been in tandem with the development of new, more effective ligands for the reaction. The combination of quantum chemical calculations and direct spectroscopic observation of catalytic intermediates has proved powerful in this regard.