RESUMEN
There is an urgent need for new antibiotics to treat multidrug-resistant Neisseria gonorrhoeae In this report, the microbiology, in vivo pharmacokinetics, and efficacy of REDX05931, a representative novel tricyclic topoisomerase inhibitor, were evaluated. REDX05931 demonstrated high oral bioavailability in mice and reduced N. gonorrhoeae infection after a single dose in a mouse model of gonorrhea. These data support the potential of this series of small molecules as a new treatment for drug-resistant gonorrheal infections.
Asunto(s)
Antibacterianos/farmacología , Gonorrea/tratamiento farmacológico , Neisseria gonorrhoeae/efectos de los fármacos , Inhibidores de Topoisomerasa/farmacología , Animales , Modelos Animales de Enfermedad , Gonorrea/microbiología , Ratones , Pruebas de Sensibilidad MicrobianaRESUMEN
Using the phospholane-phosphite ligand, BOBPHOS, almost perfect regioselectivities and high enantioselectivities (up to 92% ee) are observed in Rh catalysed enantioselective hydroformylation of vinyl arenes. This can be achieved under solvent-free conditions.