期刊
MEDICINAL CHEMISTRY RESEARCH
卷 18, 期 6, 页码 407-420出版社
BIRKHAUSER BOSTON INC
DOI: 10.1007/s00044-008-9137-9
关键词
Chalcones; Synthesis; In vitro antimalarial activity; Plasmodium falciparum
资金
- University Grant Commission (UGC), New Delhi, India [F-12-19/2004]
- University of Delhi, Delhi, India
- Department of Biotechnology, Ministry of Science and Technology, Government of India
- Council of Scientific and Industrial Research (CSIR), New Delhi
Several new chalcone analogues were synthesized and evaluated as inhibitors of malaria parasite. Inhibitory activity was determined in vitro against a chloroquine-sensitive Plasmodium falciparum strain of parasites. The compound 3-(4-methoxyphenyl)-1-(4-pyrrol-1-yl-phenyl)prop-2-en-1-one was found to be the most active with 50% inhibition concentration (IC(50)) of 1.61 mu g/ml. This inhibitory concentration is comparable to a prototype phytochemical chalcone, licochalcone A, with an IC(50) of 1.43 mu g/ml. The present study suggests that small, lipophilic nitrogen heterocyclic ring A together with small hydrophobic functionality at ring B can enhance antimalarial activity. These results suggest that chalcones are a class of compounds that provides an option of developing inexpensive, synthetic therapeutic antimalarial agents in the future.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据