Synthesis and anti-inflammatory activity of natural and semisynthetic geranyloxycoumarins

被引:58
作者
Curini, M
Epifano, F
Maltese, F
Marcotullio, MC
Tubaro, A
Altinier, G
Gonzales, SP
Rodriguez, JC
机构
[1] Univ Perugia, Sez Chim Organ, Dipartimento Chim & Tecnol Farmaco, I-06123 Perugia, Italy
[2] Univ Trieste, DEMREP, I-34127 Trieste, Italy
[3] CQF, Dept Sintesis Quim, Havana 11600, Cuba
关键词
geranyloxycoumarins; collinin; auraptene; anti-inflammatory activity;
D O I
10.1016/j.bmcl.2004.02.009
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Nine new 7-geranyloxycoumarin derivatives differently substituted at position 8 were semi-synthesised. Their topical anti-inflammatory activity was evaluated using the Croton oil ear test in mice as a model of acute inflammation. Auraptene (7-geranytoxycoumarin), its 8-methoxy (collinin, 1) and 8-acetoxy derivatives (5) (1 mumol/cm(1)) provoked 50% oedema reduction, similarly to 0.25 mumol/cm(2) of the reference drug indomethacin, a nonsteroidal anti-inflammatory drug. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2241 / 2243
页数:3
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