SYNTHESIS OF ACTIVE METABOLITES OF INDOLE PYRROLOTHIAZOLE PAF ANTAGONISTS

The major metabolites of indole pyrrolothiazole PAF antagonist 1 were shown to be sulfoxide 2 and pyridine N-oxide 3. These compounds were g enerated in vine using either isolated hepatocytes or liver microsomes . The synthesis of N-oxide 3 was accomplished by heating pyridinium sa lt 5 with hydroxylamine. Pyridine N-oxide 3 was determined to be a pot ent PAF antagonsist both in vitro and in vivo.