Preparation of 2-, 3-, 4- and 7-(2-alkylcarbamoyl-1-alkylvinyl)benzo[b]furans and their BLT1 and/or BLT2 inhibitory activities

被引：61

作者：

Ando, Kumiko ^{[1
]}

Kawamura, Yoko ^{[1
]}

Akai, Yukiko ^{[1
]}

Kunitomo, Jun-ichi ^{[1
]}

Yokomizo, Takehiko ^{[2
]}

Yamashita, Masayuki ^{[3
]}

Ohta, Shunsaku ^{[3
]}

Ohishi, Takahiro ^{[4
]}

Ohishi, Yoshitaka ^{[1
]}

机构：

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

[2] Kyushu Univ, Grad Sch Med Sci, Dept Med Biochem, Fukuoka 812, Japan

[3] Kyoto Pharmaceut Univ, Kyoto 607, Japan

[4] Doshisha Univ, Grad Sch Engn, Kyoto 610, Japan

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2008年 / 6卷 / 02期

关键词：

D O I：

10.1039/b710935k

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Several 2-alkylcarbamoyl-1-alkylvinylbenzo[b]furans were designed to find a selective leukotriene B-4 (LTB4) receptor antagonist. 2-(2-Alkylcarbamoyl-1-alkylvinyl) benzo[b] furans having a substituent group at the 3-position, 4-(2-alkylcarbamoyl-1-methylvinyl) benzo[b] furans having a substituent group at the 3-position, and 7-(2-alkylcarbamoyl-1-methylvinyl) benzo[b] furans and 3-(2-alkylcarbamoyl-1-alkylvinyl) benzo[b] furans were prepared and evaluated for LTB4 receptor (BLT1 and BLT2) inhibitory activities. (E)-3-Amino-4-[2-[2-(3,4-dimethoxyphenyl)ethylcarbamoyl]-1-methylvinyl]benzo[b]furan ((E)-17c) showed potent and selective inhibitory activity for BLT2. On the other hand, (E)-7-(2-diethylcarbamoyl-1-methylvinyl) benzo[ b] furan ((E)-27a) showed potent inhibitory activity for both BLT1 and BLT2.

引用

页码：296 / 307

页数：12

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