803684-65-3Relevant academic research and scientific papers
Preparation of 2- And 4-(2-alkylcarbamoyl-1-methylvinyl)-7-alkyloxybenzo[b]furans having potent antagonistic activity against human leukotriene B4 BLT1 and/or BLT2 receptors
Ando, Kumiko,Tsuji, Eriko,Ando, Yuko,Kunitomo, Jun-Ichi,Yamashita, Masayuki,Ohta, Shunsaku,Nabe, Takeshi,Kohno, Shigekatsu,Yokomizo, Takehiko,Shimizu, Takao,Ohishi, Yoshitaka
, p. 3427 - 3431 (2004)
(E)-2- Acetyl-4-(2-diethylcarbamoyl-1-methylvinyl)-7-(1-phenylethoxy)benzo[b]furan (4b) with a characteristic conformation and (E)-2-(2-morpholinocarbo-1-methyl-vinyl)-7-ethoxycarbopropoxybenzo[b]furan ((E)-3b) were prepared and evaluated for their leukot
BENZOFURAN COMPOUND AND MEDICINAL COMPOSITION CONTAINING THE SAME
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Page/Page column 44, (2008/06/13)
The present invention relates to a benzofuran compound of the formula (I) wherein each symbol is as defined in the description, a pharmaceutically acceptable salt thereof and the like. The compound of the present invention has superior leukotriene inhibitory action, BLT2 competitive inhibitory action, BLT2 blocking action, action for the prophylaxis or treatment of allergy, action for the prophylaxis or treatment of asthma and action for the prophylaxis or treatment of inflammation, and is useful as an agent for the prophylaxis or treatment of diseases such as allergic disease, asthma, inflammation and the like, and other diseases.
Synthesis of 2-, 4- And 5-(2-alkylcarbamoyl-l-methylvinyl)-7- alkyloxybenzo[b]furans and their leukotriene 64 receptor antagonistic activity
Ando, Kumiko,Tsuji, Eriko,Ando, Yuko,Kunitomo, Jun-Ichi,Kobayashi, Reina,Yokomizo, Takehiko,Shimizu, Takao,Yamashita, Masayuki,Ohta, Shunsaku,Nabe, Takeshi,Kohno, Shigekatsu,Ohishi, Yoshitaka
, p. 2129 - 2139 (2007/10/03)
Variable benzo[6]furan derivatives having (E)- and (Z)-2-alkylcarbamoyl-l- methylvinyl groups at the 2-, 4- and 5-positions and a carboxylpropoxy or (1-phenyl)ethoxy group at the 7-position were prepared to find novel and selective leukotriene B4 (LTB4) receptor antagonists. (E)-2-(2-Diethylcarbamoyl- l-methylvinyl)-7-(1-phenylethoxy)benzo[b]furan (4v) showed selective inhibition to the human BLT2 receptor (hBLT2). On the other hand, (E)-2-acetyl-4-(2-diethylcarbamoyl-l-methylvinyl)-7-(l-phenylethoxy)benzo[b] furan (7v) inhibited both human BLTi receptor (hBLT1) and hBLT 2. The (E)-2-(2-diethylcarbamoyl-l-methylvinyl) group lay on approximately the same plane as the benzo[e]furan ring, whereas the (E)-4-(2-diethylcarbamoyl-l-methylvinyl) group had the torsion angle (45.7°) from the benzo[e]furan ring plane. However, the (Z)-(2-alkylcarbamoyl-l- methylvinyl)benzo[b]furans were inactive. The inhibitory activity depended on the conformation of the 2-diethylcarbamoyl-l-methylvinyl group. The Royal Society of Chemistry 2005.
