Metabolism of the antimycotic agent, croconazole, in rabbits.

The biotransformation of croconazole, a potent new antimycotic agent, was studied in the rabbit. Croconazole was excreted in the urine primarily as conjugates. Most of the radioactive metabolites in the urine could be extracted with organic solvent after hydrolysis with beta-glucuronidase. As many as 16 metabolites in the organic extracts were separated by TLC. Thirteen were identified by comparison of their mass and/or proton NMR spectra with those of synthetic samples. Aromatic ring hydroxylation of each benzene ring, O-dechlorobenzylation, and loss of the imidazole ring were found to occur.