Fungal biotransformation of the antihistamine azatadine by Cunninghamella elegans.
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.
Zhang
D
D
Division of Microbiology, Food and Drug Administration, Jefferson, Arkansas 72079, USA.
Hansen
E B
EB
Deck
J
J
Heinze
T M
TM
Sutherland
J B
JB
Cerniglia
C E
CE
D001711:Biotransformation; D003533:Cyproheptadine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D005658:Fungi / Q000378:metabolism*; D006634:Histamine H1 Antagonists / Q000493:pharmacokinetics*
D006634:Histamine H1 Antagonists; D003533:Cyproheptadine; C006656:azatadine