The Metabolism of a New Schistosomicide 2-Isopropylaminomethyl-6-methyl-7-nitro-1,2,3,4-tetrahydroquinoline (UK 3883)

Abstract

1. The metabolism of a new schistosomicide, 2-isopropylaminomethyl-6-methyl-7-nitro-1,2,3,4-tetrahydroquinoline, was investigated in the mouse, rat, rabbit and rhesus monkey.2. All the species studied converted the compound to its 6-hydroxymethyl analogue, which showed greater schistosomicidal activity in vivo than the parent drug.3. Several other metabolites were also produced by oxidation at the 2- and/or 6-positions to give carboxylic acid derivatives. None of these metabolites showed biological activity.4. A species difference was apparent, since the 2-carboxylic acid metabolite was not detected in the urine or bile of the rat.