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Chirality of azelastine and flezelastine: Investigation of their enantiomers
Author(s) -
Fleischhauer Ilona,
Kutscher Bernhard,
Engel Jürgen,
AchterrathTuckermann Ute,
Borbe Harald O.,
Schmidt Jürgen,
Szelenyi Istvan,
Camuglia Giancarlo
Publication year - 1993
Publication title -
chirality
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.43
H-Index - 77
eISSN - 1520-636X
pISSN - 0899-0042
DOI - 10.1002/chir.530050517
Subject(s) - chemistry , azelastine , enantiomer , diastereomer , chirality (physics) , stereospecificity , stereochemistry , in vivo , pharmacology , organic chemistry , chiral symmetry breaking , catalysis , medicine , physics , microbiology and biotechnology , quantum mechanics , nambu–jona lasinio model , biology , quark
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.