Preparation of 2-, 3-, 4- and 7-(2-alkylcarbamoyl-1-alkylvinyl)benzo[b]furans and their BLT1 and/or BLT2 inhibitory activities
Preparation of 2-, 3-, 4- and 7-(2-alkylcarbamoyl-1-alkylvinyl)benzo[b]furans and their BLT1 and/or BLT2 inhibitory activities
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DOI：
10.1039/b710935k
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发表时间：
2008-01-01
影响因子：
3.2
通讯作者：
Ohishi, Yoshitaka
中科院分区：
文献类型：
--
作者：
Ando, Kumiko;Kawamura, Yoko;Ohishi, Yoshitaka
设计了几个2-烷基氨基甲酰基-1-烷基乙烯基苯并[B]呋喃类化合物，以寻找选择性的白三烯B-4（LTB 4）受体拮抗剂。2-在3-位上具有取代基的（2-烷基氨基甲酰基-1-烷基乙烯基）苯并[B]呋喃，4-在3位上具有取代基的（2-烷基氨基甲酰基-1-甲基乙烯基）苯并[B]呋喃，和7-（2-烷基氨基甲酰基-1-甲基乙烯基）苯并[B]呋喃和3-制备（2-烷基氨基甲酰基-1-烷基乙烯基）苯并[B]呋喃并评价其LTB 4受体（BLT 1和BLT 2）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）-17 c））对BLT 2显示出有效的选择性抑制活性。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）-27 a）对BLT 1和BLT 2均显示出有效的抑制活性。
Several 2-alkylcarbamoyl-1-alkylvinylbenzo[b]furans were designed to find a selective leukotriene B-4 (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 LTB4 receptor (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.