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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| Authors: | Sakata Yoko Kuramoto Mari Ando Kumiko Yamaguchi Mami Kawasaki Ikuo Kunitomo Jun-Ichi Yokomizo Takehiko Ohishi Yoshitaka |
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| Institution: | School of Pharmaceutical Sciences, Mukogawa Women's University, Nishinomiya, Japan. |
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| Abstract: | A series of 3-(4-chlorophenyl)-2-(2-aminothiazol-4-yl)benzob]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-methoxybenzob]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. |
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