2-Phenyl-3-(quinolizidin-1-yl)-5-substituted indoles as platelet antiaggregating agents.
作者： Vito Boido , Fabio Sparatore , Ugo Armani , Antonietta Piana , Marcella Ercoli
DOI: 10.1016/J.FARMAC.2003.11.009
关键词:
摘要: Abstract A set of ten 2-phenyl-3-(quinolizidin-1-yl)-5-substituted indoles was prepared through the Fischer cyclization lupinyl- and epi -lupinylphenylketone 4-substituted phenylhydrazones.Compounds were tested for antiaggregating activity on human platelets activated by adenosine diphosphate (ADP), collagen adrenaline. At 2.5 × 10 –4 M concentration most compounds strongly inhibited aggregation induced all agonists considered many them still displayed good at 0.625 × concentration. The least active ( 1c ) one 1d also rabbit ADP, PAF sodium arachidonate. Both against ADP PAF, but only arachidonate-induced (100% 8 × –6 concentration) increased bleeding time in mice. same subjected to a general pharmacological screening found display several activities; particular interest dose dependent reduction serum cholesterol heparin precipitating betalipoproteins hypercholesterolemic mice exerted , which significant oral 10 mg/kg.
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