CHIRALITY OF AZELASTINE AND FLEZELASTINE - INVESTIGATION OF THEIR ENANTIOMERS

Authors
FLEISCHHAUER I KUTSCHER B ENGEL J ACHTERRATHTUCKERMANN U BORBE HO SCHMIDT J SZELENYI I CAMUGLIA G
Citation
I. Fleischhauer et al., CHIRALITY OF AZELASTINE AND FLEZELASTINE - INVESTIGATION OF THEIR ENANTIOMERS, Chirality, 5(5), 1993, pp. 366-369
Citations number
6
Categorie Soggetti
Pharmacology & Pharmacy",Chemistry
Journal title
Chirality → ACNP
ISSN journal
08990042
Volume
5
Issue
5
Year of publication
1993
Pages
366 - 369
Database
ISI
SICI code
0899-0042(1993)5:5<366:COAAF->2.0.ZU;2-K
Abstract
The racemic phthalazinone derivatives azelastine and flezelastine were resolved via formation of diastereomeric salts and fractional crystal lization 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 diffe rences. However, chiral discrimination could not be observed with rega rd to overall activity of azelastine and flezelastine. (C) 1993 Wiley- Liss, Inc.