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Structure-activity relationships of kadsurenone analogues.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 1987-01-01 , DOI: 10.1021/jm00384a023 M M Ponpipom , R L Bugianesi , D R Brooker , B Z Yue , S B Hwang , T Y Shen
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 1987-01-01 , DOI: 10.1021/jm00384a023 M M Ponpipom , R L Bugianesi , D R Brooker , B Z Yue , S B Hwang , T Y Shen
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.
中文翻译:
Kadsurenone类似物的构效关系。
Kadsurenone是一种血小板活化因子(PAF)的特异性受体拮抗剂,其类似物是由肉桂醇和(烯丙氧基)苯酚的衍生物制备的。外消旋的kadsurenone,在低温下可通过Chiralpak色谱柱分离,IC50值为2 X 10(-7)M,约为天然产物活性的50%(IC50 = 1 X 10(-7)M) 。DENudatin B,mirrandin A,desallylkadsurenone和kadsurenone的2-epimer的低PAF受体阻断活性进一步证明了kadsurenone的结构特异性。
更新日期:2019-11-01
中文翻译:
![](https://scdn.x-mol.com/jcss/images/paperTranslation.png)
Kadsurenone类似物的构效关系。
Kadsurenone是一种血小板活化因子(PAF)的特异性受体拮抗剂,其类似物是由肉桂醇和(烯丙氧基)苯酚的衍生物制备的。外消旋的kadsurenone,在低温下可通过Chiralpak色谱柱分离,IC50值为2 X 10(-7)M,约为天然产物活性的50%(IC50 = 1 X 10(-7)M) 。DENudatin B,mirrandin A,desallylkadsurenone和kadsurenone的2-epimer的低PAF受体阻断活性进一步证明了kadsurenone的结构特异性。