NEW LEUKOTRIENE-B4 RECEPTOR ANTAGONIST - LEUCETTAMINE-A AND RELATED IMIDAZOLE ALKALOIDS FROM THE MARINE SPONGE LEUCETTA-MICRORAPHIS

被引:127
作者
CHAN, GW
MONG, S
HEMLING, ME
FREYER, AJ
OFFEN, PH
DEBROSSE, CW
SARAU, HM
WESTLEY, JW
机构
[1] Research and Development, SmithKline Beecham Pharmaceuticals, Pennsylvania 19406-0939, PO Box 1539, King of Prussia
来源
JOURNAL OF NATURAL PRODUCTS | 1993年 / 56卷 / 01期
关键词
D O I
10.1021/np50091a016
中图分类号
Q94 [植物学];
学科分类号
071001 ;
摘要
Three new imidazole alkaloids, leucettamines A [l] and B [2] and leucettamidine [3], have been isolated from the Palauan sponge Leucetta microraphis. Their structures were established on the basis of extensive spectral analyses. Leucettamine A showed potent leukotriene B, receptor binding activity (K(i) = 1.3 muM), while leucettamine B was essentially inactive (K(i) = 100 muM) and leucettamidine showed significant activity (K(i) = 5.3 muM). With leucettamine A identified as a pure LTB4 receptor antagonist, a new structure lead is presented to inflammation therapy.
引用
收藏
页码:116 / 121
页数:6
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