Preparation of Benzo[b]furans Having Five-Membered Heterocycles at the 2-Position and 2-(4-Alkylcarbamoylbuta-1,3-dienyl)benzo[b]furans, and Their Cysteinyl Leukotriene Receptor (cysLT1, cysLT2) Inhibitory Activity

Yukiko Akai; Yukako Tabuchi; Kumiko Ando; Azusa Ito; Yoko Sakata; Ikuo Kawasaki; Takahiro Ohishi; Masayuki Yamashita; Shunsaku Ohta; Kiyoharu Nishide; Yoshitaka Ohishi

doi:10.1248/cpb.c12-00560

Notes

Preparation of Benzo[b]furans Having Five-Membered Heterocycles at the 2-Position and 2-(4-Alkylcarbamoylbuta-1,3-dienyl)benzo[b]furans, and Their Cysteinyl Leukotriene Receptor (cysLT1, cysLT2) Inhibitory Activity

Yukiko Akai, Yukako Tabuchi, Kumiko Ando, Azusa Ito, Yoko Sakata, Ikuo Kawasaki, Takahiro Ohishi, Masayuki Yamashita, Shunsaku Ohta, Kiyoharu Nishide, Yoshitaka Ohishi

Author information

Yukiko Akai
School of Pharmaceutical Sciences, Mukogawa Women’s University
Yukako Tabuchi
School of Pharmaceutical Sciences, Mukogawa Women’s University
Kumiko Ando
School of Pharmaceutical Sciences, Mukogawa Women’s University
Azusa Ito
School of Pharmaceutical Sciences, Mukogawa Women’s University
Yoko Sakata
School of Pharmaceutical Sciences, Mukogawa Women’s University
Ikuo Kawasaki
School of Pharmaceutical Sciences, Mukogawa Women’s University
Takahiro Ohishi
Science of Environment and Mathematical Modeling, Graduate School of Engineering, Doshisha University
Masayuki Yamashita
Kyoto Pharmaceutical University
Shunsaku Ohta
Kyoto Pharmaceutical University
Kiyoharu Nishide
School of Pharmaceutical Sciences, Mukogawa Women’s University
Yoshitaka Ohishi
School of Pharmaceutical Sciences, Mukogawa Women’s University
Doshisha Women’s College of Liberal Arts

Keywords: benzo[b]furan, cysteinyl leukotriene receptor inhibitory activity, heterocycle

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Supplementary material

2012 Volume 60 Issue 11 Pages 1461-1467

DOI https://doi.org/10.1248/cpb.c12-00560

Details

Abstract

A series of benzo[b]furan derivatives having a five-membered heterocyclic substituent at the 2-position were prepared from 2-(1-chloro-2-formylvinyl)benzo[b]furans (2) and 2-(4-alkylcarbamoylbuta-1,3-dienyl)benzo[b]furans. These 2-heterocyclic benzo[b]furans were evaluated for their cysteinyl leukotriene receptor (cysLT1, cysLT2) inhibitory activity. Several compounds showed moderate inhibition of calcium mobilization in HEK 293T-cysLT2 or CHO-cysLT1 cells.

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