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Appl. Environ. Microbiol., Sep 1996, 3477-3479, Vol 62, No. 9
Copyright © 1996, American Society for Microbiology

Fungal biotransformation of the antihistamine azatadine by Cunninghamella elegans

D Zhang, EB Hansen Jr, J Deck, TM Heinze, JB Sutherland and CE Cerniglia
Division of Microbiology, Food and Drug Administration, Jefferson, Arkansas 72079, USA.

The metabolism of the antihistamine azatadine by the zygomycete fungus Cunninghamella elegans ATCC 9245 was investigated. Within 72 h from the addition of the drug to 48-h-old cultures grown in Sabouraud dextrose broth, 95% of azatadine was biotransformed. Two major metabolites, 7- hydroxyazatadine (25%) and 8-hydroxyazatadine (50%), and two minor metabolites, N-desmethylazatadine and 9-hydroxyazatadine, were isolated by high-performance liquid chromatography and characterized by mass spectrometric and proton nuclear magnetic resonance spectroscopic analyses.

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