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Chirality of azelastine and flezelastine: Investigation of their enantiomers
Authors:Ilona Fleischhauer  Bernhard Kutscher  Jürgen Engel  Ute Achterrath-Tuckermann  Harald O Borbe  Jürgen Schmidt  Istvan Szelenyi  Giancarlo Camuglia
Abstract:The racemic phthalazinone derivatives azelastine and flezelastine were resolved via formation of diastereomeric salts and fractional crystallization thereof. The optical purity of the enantiomers was checked by HPLC. Pharmacological investigations in vitro and in vivo related to antiallergic/antiasthmatic activity revealed some stereospecific differences. However, chiral discrimination could not be observed with regard to overall activity of azelastine and flezelastine. © 1993 Wiley-Liss, Inc.
Keywords:azelastine  flezelastine  fractional crystallization  antiallergic/antiasthmatic  chiral discrimination
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