SYNTHESIS OF CHIRAL AND ACHIRAL PYRANENAMINE DERIVATIVES - POTENT AGENTS WITH TOPICAL OCULAR ANTIALLERGIC ACTIVITY

被引：5

作者：

GLUCHOWSKI, C

BISCHOFF, TE

GARST, ME

KAPLAN, LJ

DIETRICH, SW

ASWAD, AS

GAFFNEY, MA

AOKI, KR

GARCIA, C

WHEELER, LA

机构：

[1] ALLERGAN PHARMACEUT INC,DEPT CHEM,IRVINE,CA 92715

[2] ALLERGAN PHARMACEUT INC,DEPT BIOL SCI,IRVINE,CA 92715

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1991年 / 34卷 / 01期

关键词：

D O I：

10.1021/jm00105a060

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The SS, RR and meso stereoisomers of pyranenamine SK&F 84210 (2) were synthesized stereospecifically starting from commercially available (R)-(-)- or (S)-(+)-2,2-dimethyl-1,3,dioxolane-4-methanol (3). In addition, two achiral pyranenamines 19 and 26 were also synthesized. When evaluated by intravenous and topical routes in the rat passive ocular anaphylaxis (POA) assay, (SS)- and meso-2 as well as achiral compounds 19 and 26 were found to be more potent antiallergic agents than (RR)-2.

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页码：392 / 397

页数：6

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