RESUMO
We describe here the synthesis and biological evaluation of a series of benzo[b]naphthyridones, a new family of tricyclic antibacterial compounds that have a gram-positive spectrum of activity. RP60556A, one of the most potent of these compounds, is bactericidal against multiresistant cocci, especially multiresistant Staphylococcus aureus strains. Its physico-chemical and biological properties make it particularly suitable for topical antibacterial use.
Assuntos
Anti-Infecciosos Locais/farmacologia , Resistência a Múltiplos Medicamentos , Bactérias Gram-Positivas/efeitos dos fármacos , Naftiridinas/síntese química , Naftiridinas/farmacologia , Piperazinas/síntese química , Piperazinas/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Animais , Antibacterianos/síntese química , Antibacterianos/farmacologia , Anti-Infecciosos Locais/síntese química , Avaliação Pré-Clínica de Medicamentos , Cobaias , Testes de Sensibilidade Microbiana , Infecções Cutâneas Estafilocócicas/tratamento farmacológicoRESUMO
A flavone, jaceosidine, and a sesquiterpene lactone, cynaropicrine, have been isolated from the aerial parts and flowers of Volutarella divaricata. The structures were established by chemical (acetylation, saponification, formylation) and spectroscopic methods (I.R., U.V., R.M.N., Mass spectra). This is the first report of these products from this plant.
RESUMO
From leaves, root - and stem - barks of Annona muricata L., seven isoquinoline alkaloids have been isolated: reticuline (main alkaloid), coclaurine, coreximine, atherosperminine, stepharine. Anomurine and anomuricine, two minor alkaloids, are new tetrahydrobenzylisoquinolines, with 5, 6, 7 substituted ring A. The phytochemical significance of these alkaloids is discussed.
