Metabolic pathway by cleavage of a furan ring

Abstract

1. ¹⁴C-Diclofurime, a new Ca antagonist, was administered orally to dogs and pigs, and metabolites detected in urine and plasma.

2. Metabolites contained in pooled urine were concentrated by column chroma-tography (reverse phase, gel permeation and normal phase). Chemical structures were determined by i.r. mass and ¹H n.m.r. spectroscopy.

3. The main route of Diclofurime biotransformation involved cleavage of the furan ring. Subsequent biotransformation steps involved N-deethylation in the side-chain and O-demethylation in the aromatic moiety of the drug.

4. The major pathway is unusual for molecules with a furan heterocycle.