Preparation of 3-(4-chlorophenyl)-2-(2-aminothiazol-4-yl)-5-methoxybenzo[b]furan derivatives and their leukotriene B4 inhibitory activity

Yoko Sakata; Mari Kuramoto; Kumiko Ando; Mami Yamaguchi; Ikuo Kawasaki; Jun-ichi Kunitomo; Takehiko Yokomizo; Yoshitaka Ohishi

doi:10.1039/B711391A

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Preparation of 3-(4-chlorophenyl)-2-(2-aminothiazol-4-yl)-5-methoxybenzo[b]furan derivatives and their leukotriene B₄ inhibitory activity†

Yoko Sakata,^a Mari Kuramoto,^a Kumiko Ando,^a Mami Yamaguchi,^a Ikuo Kawasaki,^a Jun-ichi Kunitomo,^a Takehiko Yokomizo^b and Yoshitaka Ohishi*^a

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* Corresponding authors

^a School of Pharmaceutical Sciences, Mukogawa Women's University, 11-68, Koshien Kyuban-cho, Nishinomiya, Japan
E-mail: yohishi@mukogawa-u.ac.jp
Fax: +798 45 9953
Tel: +798 45 9953

^b Department of Medical Biochemistry, Graduate School of Medical Sciences, Kyushu University, Maidashi 3-1-1, Higashi-ku, Fukuoka, Japan

Abstract

A series of 3-(4-chlorophenyl)-2-(2-aminothiazol-4-yl)benzo[b]furan derivatives 6–10 were prepared and their leukotriene B₄ inhibitory activity was evaluated. We found that several compounds showed strong inhibition of calcium mobilization in CHO cells overexpressing human BLT₁ and BLT₂ receptors. Among them, 3-(4-chlorophenyl)-2-[5-formyl-2-[(dimethylamino)methyleneamino]thiazol-4-yl]-5-methoxybenzo[b]furan9b showed the most potent and selective inhibition for the human BLT₂ receptor, and its IC₅₀ value was smaller than that of the selected positive control compound, ZK-158252.

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Supplementary files

Physical and experimental detail for 9a, 10a and 10b PDF (40K)

Article information

DOI: https://doi.org/10.1039/B711391A
Article type: Communication
Submitted: 25 Jul 2007
Accepted: 21 Aug 2007
First published: 31 Aug 2007

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Org. Biomol. Chem., 2007,5, 3083-3086

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Preparation of 3-(4-chlorophenyl)-2-(2-aminothiazol-4-yl)-5-methoxybenzo[b]furan derivatives and their leukotriene B₄ inhibitory activity

Y. Sakata, M. Kuramoto, K. Ando, M. Yamaguchi, I. Kawasaki, J. Kunitomo, T. Yokomizo and Y. Ohishi, Org. Biomol. Chem., 2007, 5, 3083 DOI: 10.1039/B711391A

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Organic & Biomolecular Chemistry