Preparation of 3-(4-chlorophenyl)-2-(2-aminothiazol-4-yl)-5-methoxybenzo[b]furan derivatives and their leukotriene B(4) inhibitory activity.
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.
Sakata
Yoko
Y
School of Pharmaceutical Sciences, Mukogawa Women's University, Nishinomiya, Japan.
Kuramoto
Mari
M
Ando
Kumiko
K
Yamaguchi
Mami
M
Kawasaki
Ikuo
I
Kunitomo
Jun-Ichi
J
Yokomizo
Takehiko
T
Ohishi
Yoshitaka
Y
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
D001572:Benzofurans; D007975:Leukotriene B4