Preparation of 3-(4-chlorophenyl)-2-(2-aminothiazol-4-yl)-5-methoxybenzo[b]furan derivatives and their leukotriene B(4) inhibitory activity.
Preparation of 3-(4-chlorophenyl)-2-(2-aminothiazol-4-yl)-5-methoxybenzo[b]furan derivatives and their leukotriene B(4) inhibitory activity.
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DOI：
10.1039/b711391a
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发表时间：
2007-09
影响因子：
3.2
通讯作者：
Y. Sakata;Mari Kuramoto;Kumiko Ando;Mami Yamaguchi;I. Kawasaki;J. Kunitomo;T. Yokomizo;Y. Ohishi
中科院分区：
文献类型：
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作者：
Y. Sakata;Mari Kuramoto;Kumiko Ando;Mami Yamaguchi;I. Kawasaki;J. Kunitomo;T. Yokomizo;Y. Ohishi
制备了一系列3-(4-氯苯基)-2-(2-氨基噻唑-4-基)苯并[b]呋喃衍生物6-10并评价了它们的白三烯B(4)抑制活性。我们发现，几种化合物对过表达人 BLT(1) 和 BLT(2) 受体的 CHO 细胞中的钙动员表现出强烈的抑制作用。其中，3-(4-氯苯基)-2-[5-甲酰基-2-[(二甲氨基)亚甲基氨基]噻唑-4-基]-5-甲氧基苯并[b]呋喃9b对人BLT(2)受体表现出最有效和选择性的抑制作用，其IC(50)值小于所选阳性对照化合物ZK-158252。
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 BLT(1) and BLT(2) 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 BLT(2) receptor, and its IC(50) value was smaller than that of the selected positive control compound, ZK-158252.