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) recept...

Full description

Saved in:
Bibliographic Details
Published in:Organic & biomolecular chemistry 2007-10, Vol.5 (19), p.3083-3086
Main Authors: Sakata, Yoko, Kuramoto, Mari, Ando, Kumiko, Yamaguchi, Mami, Kawasaki, Ikuo, Kunitomo, Jun-Ichi, Yokomizo, Takehiko, Ohishi, Yoshitaka
Format: Article
Language:English
Subjects:
Animals
Benzofurans - chemical synthesis
Benzofurans - pharmacology
CHO Cells
Cricetinae
Cricetulus
Humans
Leukotriene B4 - antagonists & inhibitors
Structure-Activity Relationship
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:1477-0520