Author/Authors :
Steven K. Davidsen، نويسنده , , James B. Summers، نويسنده , , David J. Sweeny، نويسنده , , James H. Holms، نويسنده , , Daniel H. Albert، نويسنده , , George M. Carrera Jr.، نويسنده , , Paul Tapang، نويسنده , , Terrance J. Magoc، نويسنده , , Richard G. Conway، نويسنده , , David A. Rhein، نويسنده ,
Abstract :
The major metabolites of indole pyrrolothiazole PAF antagonist 1 were shown to be sulfoxide 2 and pyridine N-oxide 3. These compounds were generated in vitro using either isolated hepatocytes or liver microsomes. The synthesis of N-oxide 3 was accomplished by heating pyridinium salt 5 with hydroxylamine. Pyridine N-oxide 3 was determined to be a potent PAF antagonsist both in vitro and in vivo.
