3-(4-氯苯基)-2-(2-氨基噻唑-4-基)-5-甲氧基苯并[b]呋喃衍生物的制备及其白三烯B(4)抑制活性
Preparation of 3-(4-chlorophenyl)-2-(2-aminothiazol-4-yl)-5-methoxybenzo[b]furan derivatives and their leukotriene B(4) inhibitory activity.
作者信息
Sakata Yoko, Kuramoto Mari, Ando Kumiko, Yamaguchi Mami, Kawasaki Ikuo, Kunitomo Jun-Ichi, Yokomizo Takehiko, Ohishi Yoshitaka
机构信息
School of Pharmaceutical Sciences, Mukogawa Women's University, Nishinomiya, Japan.
出版信息
Org Biomol Chem. 2007 Oct 7;5(19):3083-6. doi: 10.1039/b711391a. Epub 2007 Aug 31.
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.
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，并评估了它们对白三烯B(4)的抑制活性。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抑制作用。其中，3-(4-氯苯基)-2-[5-甲酰基-2-[(二甲基氨基)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的IC(50)值。
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