CHIRALITY OF AZELASTINE AND FLEZELASTINE - INVESTIGATION OF THEIR ENANTIOMERS

被引：7

作者：

FLEISCHHAUER, I

KUTSCHER, B

ENGEL, J

ACHTERRATHTUCKERMANN, U

BORBE, HO

SCHMIDT, J

SZELENYI, I

CAMUGLIA, G

机构：

[1] ASTA MED AG,DEPT BIOCHEM,FRANKFURT,GERMANY

[2] ASTA MED AG,DEPT PHARMACOL,FRANKFURT,GERMANY

[3] ASTA MED AG,DEPT ANALYT,FRANKFURT,GERMANY

来源：

CHIRALITY | 1993年 / 5卷 / 05期

关键词：

AZELASTINE; FLEZELASTINE; FRACTIONAL CRYSTALLIZATION; ANTIALLERGIC/ANTIASTHMATIC; CHIRAL DISCRIMINATION;

D O I：

10.1002/chir.530050517

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 1993 Wiley-Liss, Inc.

引用

页码：366 / 369

页数：4

共 6 条

[1] EVIDENCE FOR LOW BRAIN PENETRATION BY THE H-1-RECEPTOR ANTAGONIST TEMELASTINE (SK-AND-F-93944) [J].