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Structure-activity relationships of kadsurenone analogues.

Abstract：

:Kadsurenone, a specific receptor antagonist of platelet-activating factor (PAF), and its analogues were prepared from derivatives of cinnamyl alcohol and (allyloxy)phenol. Racemic kadsurenone, resolvable by a Chiralpak column at low temperatures, has an IC50 value of 2 X 10(-7) M, which is about 50% of the activity of the natural product (IC50 = 1 X 10(-7) M). The structural specificity of kadsurenone was further demonstrated by the low PAF-receptor-blocking activities of denudatin B, mirandin A, desallylkadsurenone, and the 2-epimer of kadsurenone.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Ponpipom MM,Bugianesi RL,Brooker DR,Yue BZ,Hwang SB,Shen TY

doi

10.1021/jm00384a023

subject

Has Abstract

pub_date

1987-01-01 00:00:00

pages

136-42

issue

1

eissn

0022-2623

issn

1520-4804

journal_volume

30

pub_type

杂志文章

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