RESUMO
In order to obtain self assembling, multivalent ligand for influenza virus hemagglutinin α-N-acetylneuraminyl-(2-6)-D-galactopyranose has been synthesized and bonded to a water soluble fullerene derivative using 1,3-dipolar cycloaddition click reaction. The aggregating amphiphilic compound did not inhibit the influenza virus hemagglutinin, but it proved to be an inhibitor of its neuraminidase with a 50% inhibitory concentration of 81 µM.
Assuntos
Hidrocarbonetos Aromáticos com Pontes/farmacologia , Dissacarídeos/farmacologia , Fulerenos/farmacologia , Hemaglutininas/metabolismo , Neuraminidase/antagonistas & inibidores , Orthomyxoviridae/metabolismo , Hidrocarbonetos Aromáticos com Pontes/síntese química , Hidrocarbonetos Aromáticos com Pontes/química , Dissacarídeos/síntese química , Dissacarídeos/química , Relação Dose-Resposta a Droga , Fulerenos/química , Ligantes , Estrutura Molecular , Neuraminidase/metabolismo , Orthomyxoviridae/efeitos dos fármacos , Relação Estrutura-AtividadeRESUMO
Glycopeptide antibiotic derivative teicoplanin ψ-aglycone has been bound covalently to a fullerenopyrrolidine derivative using azide-alkyne 1,3-dipolar cycloaddition reaction. The aggregation of the antibiotic-fullerene conjugate in aqueous solution has been studied. The conjugate exhibited antibacterial activity against enterococci resistant to teicoplanin.
Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Fulerenos/química , Teicoplanina/análogos & derivados , Antibacterianos/síntese química , Bactérias/efeitos dos fármacos , Técnicas de Química Sintética , Teicoplanina/químicaRESUMO
1-Hydroxybisphosphonate derivatives of ciprofloxacin, gatifloxacin and moxifloxacin have been synthesized using Cu(I) catalyzed azide-alkyne 1,3-dipolar cycloaddition reaction. The 1,2,3-triazol linked hydroxybisphosphonate derivative of ciprofloxacin exhibited antibacterial activity comparable to the parent antibiotic and all fluoroquinolone-bisphosphonates displayed osteotropic properties in a bone model.