Synthesis of active metabolites of indole pyrrolothiazole paf antagonists

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 .