The interaction of arylalkylbenzimidazoles and related compounds with microsomal oxidation

Abstract

1. A series of 2-arylalkyl- and 2-(4′-alkyl)phenoxymethylbenzimidazoles was synthesized and evaluated as inhibitors of mixed-function oxidase activity in phenobarbitone- and β-naphthoflavone-induced rat liver microsomes.

2. Higher homologues of the 2-arylalkyl series were more potent inhibitors than lower homologues against all mono-oxygenase activities except aniline p-hydroxylation.

3. Smaller 2-substituents were associated with relatively low-affinity reverse type I spectral binding behaviour, whereas larger substituents were associated with type I binding of high affinity.