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Xenobiotica
the fate of foreign compounds in biological systems
Volume 2, 1972 - Issue 2
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Research Article

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

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Pages 169-178 | Received 09 Nov 1971, Published online: 22 Sep 2008
 

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.

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