降新木脂素的抗疟及抗疟原虫活性。合成与构效关系。

Antimalarial and antiplasmodial activities of norneolignans. Syntheses and SAR.

作者信息

Skytte Dorthe Mondrup, Nielsen Simon Feldbaek, Chen Ming, Zhai Lin, Olsen Carl Erik, Christensen Søren Brøgger

机构信息

Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, Universitetsparken 2, DK-2100 Copenhagen Ø, Denmark.

出版信息

J Med Chem. 2006 Jan 12;49(1):436-40. doi: 10.1021/jm0508235.

DOI:10.1021/jm0508235

PMID:16392829

Abstract

A systematic change of the substituents and side chain of the norneolignan hinokiresinol afforded a 10 fold improvement of the IC(50) value toward inhibition of the growth of Plasmodium falciparum. The more potent compounds controlled the parasitemia in mice infected with Plasmodium berghei.

摘要

对降新木脂素扁柏脂素的取代基和侧链进行系统改变后，其对恶性疟原虫生长抑制的半数抑制浓度（IC50）值提高了10倍。效力更强的化合物可控制感染伯氏疟原虫的小鼠体内的疟原虫血症。