title: Preparation of 3-(4-chlorophenyl)-2-(2-aminothiazol-4-yl)-5-methoxybenzo[b]furan derivatives and their leukotriene B(4) inhibitory activity.
abstract: 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.
authors: School of Pharmaceutical Sciences, Mukogawa Women's University, Nishinomiya, Japan.
authors: Yoko
authors: Y
authors: Sakata
authors: Mari
authors: M
authors: Kuramoto
authors: Kumiko
authors: K
authors: Ando
authors: Mami
authors: M
authors: Yamaguchi
authors: Ikuo
authors: I
authors: Kawasaki
authors: Jun-Ichi
authors: J
authors: Kunitomo
authors: Takehiko
authors: T
authors: Yokomizo
authors: Yoshitaka
authors: Y
authors: Ohishi
mesh_terms: D000818:Animals; D001572:Benzofurans / Q000138:chemical synthesis* / Q000494:pharmacology; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D006801:Humans; D007975:Leukotriene B4 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D001572:Benzofurans; D007975:Leukotriene B4