Preparation of 2-and 4-(2-alkylcarbamoyl-1-methylvinyl)-7-alkyloxybenzo[b]furans having potent antagonistic activity against human leukotriene B4BLT1 and/or BLT2 receptors

被引：11

作者：

Ando, K

Tsuji, E

Ando, Y

Kunitomo, J

Yamashita, M

Ohta, S

Nabe, T

Kohno, S

Yokomizo, T

Shimizu, T

Ohishi, Y

机构：

[1] Mukogawa Womens Univ, Sch Pharmaceut Sci, Nishinomiya, Hyogo 6638179, Japan

[2] Kyoto Pharmaceut Univ, Kyoto 6078412, Japan

[3] Univ Tokyo, Fac Med, Dept Biochem & Mol Biol, Bunkyo Ku, Tokyo 1130033, Japan

[4] PRESTO, Tokyo 1130033, Japan

[5] JST, CREST, Bunkyo Ku, Tokyo 1130033, Japan

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2004年 / 2卷 / 23期

关键词：

D O I：

10.1039/b411286e

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

(E)-2-Acetyl-4-(2-diethylcarbamoyl-1-methylvinyl)-7-(1-phenylethoxy) benzo[b] furan (4b) with a characteristic conformation and (E)-2-(2-morpholinocarbo-1-methyl-vinyl) 7- ethoxycarbopropoxybenzo[b] furan ((E)-3b) were prepared and evaluated for their leukotriene B-4 (LTB4) antagonistic activity. Compound 4b showed potent antagonistic activity against human BLT1 and BLT2 receptors. Compound (E)-3b displayed selective BLT2 receptor antagonistic activity. Both compounds were inactive to cysteinyl LT receptors.

引用

收藏

页码：3427 / 3431

页数：5

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