Croconazole metabolism in rats.
1. Following subcutaneous administration of 1-(2-(3-chlorobenzyloxy)phenyl)vinyl)-1H-imidazole (croconazole) to rats, four metabolites were identified by comparison of their mass and n.m.r. spectra, g.l.c., and t.l.c. with those of synthetic compounds and enzyme hydrolysis. These compounds are o-hydroxyacetophenone sulphate (M1S), 1-(1-(2-hydroxyphenacyl)vinyl)-1H-imidazole sulphate (M12S), 2-(3-chlorobenzyloxy)phenacyl alcohol (M2), and 2-(3-chlorobenzyloxy)benzoic acid (M9-1). 2. At 10 mg/kg dosing of croconazole the elimination rate of the unchanged drug from plasma was faster in male than in female rats. 3. The percentage of excretion of M12S in 24 h urine was 17% for males and 7.5% for females, and that of M1S was 6.6% for males and 6.5% for females. The percentage of excretion of M2 in 24 h bile was 14% for males and 22% for females, and that of M9-1 was 3.7% for males and 1.6% for females.
Nakano
M
M
Shionogi & Co. Ltd, Shionogi Research Laboratories, Osaka, Japan.
Takeuchi
M
M
Kawahara
S
S
Mizojiri
K
K
D000818:Animals; D000935:Antifungal Agents / Q000378:metabolism; D001646:Bile / Q000378:metabolism; D005260:Female; D006868:Hydrolysis; D007093:Imidazoles / Q000097:blood / Q000378:metabolism* / Q000652:urine; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013058:Mass Spectrometry; D015394:Molecular Structure; D011817:Rabbits; D051381:Rats; D013045:Species Specificity; D015262:Xenobiotics / Q000378:metabolism
D000935:Antifungal Agents; D007093:Imidazoles; D015262:Xenobiotics; C038008:croconazole