Metabolic pathways of the contragestational agent, 3-(2-ethylphenyl)-5-(3-methoxyphenyl)-lH-l, 2,4-triazole (DL 111-IT), in the rat

• DOI: 10.3109/00498258409151431
• Publication Date: 2009-09-30T15:36:24Z
• Authors: A. Assandri; A. Perazzi; P. Ferrari; A. Omodei-sale; A. Ripamonti; G. Tuan; G. Galliani; L. F. Zerilli
• Keywords: Hydroxylation; Triazole; Demethylation; Metabolic pathway

The metabolic pathways of the non-hormonal anti-fertility agent 3-(2-ethylphenyl)-5-(3-methoxyphenyl)-1H-1,2,4-triazole (DL 111-IT) were studied in rats given 14C-labelled compound intramuscularly. diaryltriazole, once absorbed, was metabolized rapidly by three phase I reactions: (a) hydroxylation at C-4 methoxyphenyl ring, (b) alpha-C ethyl chain, and (c) demethylation methoxyl function. Seven free metabolites conjugates have been isolated characterized u.v., i.r., n.m.r. mass spectroscopy. products first step metabolism diaryltriazole tested for their pregnancy-terminating activity rat. They only 5-9% as effective parent compound, indicating that unchanged drug is active molecule.