Synthesis and heme-binding correlation with antimalarial activity of 3,6-bis-(ω-N,N-diethylaminoamyloxy)-4,5-difluoroxanthone

被引：20

作者：

Dodean, Rozalia A. ^{[1
,2
]}

Kelly, Jane X. ^{[2
]}

Peyton, David ^{[1
]}

Gard, Gary L. ^{[1
]}

Riscoe, Michael K. ^{[2
]}

Winter, Rolf W. ^{[1
]}

机构：

[1] Portland State Univ, Dept Chem, Portland, OR 97207 USA

[2] VA Med Ctr, Med Res Serv, Portland, OR 97239 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2008年 / 16卷 / 03期

关键词：

D O I：

10.1016/j.bmc.2007.10.083

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

In this study, the effect of fluorine upon the heme-binding ability of the xanthone nucleus was investigated for 3,6-bis-((omega-N,N-diethylaminoamyloxy)-4,5-difluoroxanthone (F2C5). 2-Fluoro-1,3-dimethoxybenzene was prepared by a new, improved method and used to build up the xanthone nucleus. The interaction of F2C5 with heme was investigated by UV-vis, H-1 NMR, and F-19 NMR spectroscopy. For the first time, NMR studies for the heme-drug interactions are carried out at pH 5.0, physiological for the acidic food vacuole of the malaria parasite. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：1174 / 1183

页数：10

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