Journal of Medicinal Chemistry p. 136 - 142 (1987)
Update date:2022-08-02
Topics:
Ponpipom, Mitree M.
Bugianesi, Robert L.
Brooker, David R.
Yue, Bao-Zhen
Hwang, San-Bao
Shen, Tsung-Ying
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 * 10-7 M, which is about 50percent of the activity of the natural product (IC50 = 1 * 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.
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