Ando Kumiko, Tsuji Eriko, Ando Yuko, Kunitomo Jun-ichi, Yamashita Masayuki, Ohta Shunsaku, Nabe Takeshi, Kohno Shigekatsu, Yokomizo Takehiko, Shimizu Takao, Ohishi Yoshitaka
School of Pharmaceutical Sciences, Mukogawa Women's University, 11-68 Koshien Kyuban-cho, Nishinomiya, 663-8179, Japan.
Org Biomol Chem. 2004 Dec 7;2(23):3427-31. doi: 10.1039/b411286e. Epub 2004 Nov 1.
(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-methylvinyl)-7-ethoxycarbopropoxybenzo[b]furan ((E)-3b) were prepared and evaluated for their leukotriene B4(LTB4) antagonistic activity. Compound 4b showed potent antagonistic activity against human BLT1 and BLT2 receptors. Compound (E)-3b displayed selective BLT2 receptor antagonistic activity. Both compounds were inactive to cysteinyl LT receptors.
制备了具有特征构象的(E)-2-乙酰基-4-(2-二乙氨基甲酰基-1-甲基乙烯基)-7-(1-苯乙氧基)苯并[b]呋喃(4b)和(E)-2-(2-吗啉甲酰基-1-甲基乙烯基)-7-乙氧基羰基丙氧基苯并[b]呋喃((E)-3b)，并对它们的白三烯B4(LTB4)拮抗活性进行了评估。化合物4b对人BLT1和BLT2受体表现出强效拮抗活性。化合物(E)-3b表现出选择性BLT2受体拮抗活性。两种化合物对半胱氨酰白三烯受体均无活性。
