Several 2-alkylcarbamoyl-1-alkylvinylbenzo[b]furans were designed to find a selective leukotriene B4 (LTB4) receptor antagonist. 2-(2-Alkylcarbamoyl-1-alkylvinyl)benzo[b]furans having a substituent group at the 3-position, 4-(2-alkylcarbamoyl-1-methylvinyl)benzo[b]furans having a substituent group at the 3-position, and 7-(2-alkylcarbamoyl-1-methylvinyl)benzo[b]furans and 3-(2-alkylcarbamoyl-1-alkylvinyl)benzo[b]furans were prepared and evaluated for LTB4receptor (BLT1 and BLT2) inhibitory activities. (E)-3-Amino-4-[2-[2-(3,4-dimethoxyphenyl)ethylcarbamoyl]-1-methylvinyl]benzo[b]furan ((E)-17c) showed potent and selective inhibitory activity for BLT2. On the other hand, (E)-7-(2-diethylcarbamoyl-1-methylvinyl)benzo[b]furan ((E)-27a) showed potent inhibitory activity for both BLT1 and BLT2.
设计了几种2-烷基
氨基甲酰基-1-烷基
乙烯基苯并[b]
呋喃,旨在寻找选择性的
白三烯B4(LTB4)受体拮抗剂。合成了在3-位具有取代基的2-(2-烷基
氨基甲酰基-1-烷基
乙烯基)苯并[b]
呋喃、在3-位具有取代基的4-(2-烷基
氨基甲酰基-1-甲基
乙烯基)苯并[b]
呋喃、7-(2-烷基
氨基甲酰基-1-甲基
乙烯基)苯并[b]
呋喃和3-(2-烷基
氨基甲酰基-1-烷基
乙烯基)苯并[b]
呋喃,并评估了它们对LTB4受体(BLT1和BLT2)的抑制活性。(E)-3-
氨基-4-[2-[2-(3,4-二
甲氧基苯基)乙基
氨基甲酰基]-1-甲基
乙烯基]苯并[b]
呋喃((E)-17c)显示出对BLT2具有强效且选择性的抑制活性。另一方面,(E)-7-(2-
二乙基氨基甲酰基-1-甲基
乙烯基)苯并[b]
呋喃((E)-27a)对BLT1和BLT2均显示出强效的抑制活性。