Preparation of 3-(4-chlorophenyl)-2-(2-aminothiazol-4-yl)-5-methoxybenzo[b] furan derivatives and their leukotriene B4 inhibitory activity

被引:6
|
作者
Sakata, Yoko
Kuramoto, Mari
Ando, Kumiko
Yamaguchi, Mami
Kawasaki, Ikuo
Kunitomo, Jun-ichi
Yokomizo, Takehiko
Ohishi, Yoshitaka
机构
[1] Mukogawa Womens Univ, Sch Pharmaceut Sci, Nishinomiya, Hyogo 6638179, Japan
[2] Kyushu Univ, Grad Sch Med Sci, Dept Med Biochem, Higashi Ku, Fukuoka 812, Japan
关键词
D O I
10.1039/b711391a
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A series of 3-(4-chlorophenyl)-2-(2-aminothiazol-4-yl)benzo[b] furan derivatives 6-10 were prepared and their leukotriene B-4 inhibitory activity was evaluated. We found that several compounds showed strong inhibition of calcium mobilization in CHO cells overexpressing human BLT1 and BLT2 receptors. Among them, 3-(4-chlorophenyl)-2-[5-formyl-2-[(dimethylamino)methyleneamino]thiazol-4-yl]5-methoxybenzo[b]furan 9b showed the most potent and selective inhibition for the human BLT2 receptor, and its IC50 value was smaller than that of the selected positive control compound, ZK-158252.
引用
收藏
页码:3083 / 3086
页数:4
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