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新型呋喃并[2,3,4-jk][2]苯并氮杂卓-4(3H)-酮衍生物的合成及生物活性

Synthesis and biological activities of novel furo[2,3,4-jk][2]benzazepin-4(3H)-one derivatives.

作者信息

Ando Kumiko, Akai Yukiko, Kunitomo Jun-Ichi, Yokomizo Takehiko, Nakajima Hidemitsu, Takeuchi Tadayoshi, Yamashita Masayuki, Ohta Shunsaku, Ohishi Takahiro, Ohishi Yoshitaka

机构信息

School of Pharmaceutical Sciences, Mukogawa Women's University, 11-68 Koshien Kyuban-cho, Nishinomiya 663-8179, Japan.

出版信息

Org Biomol Chem. 2007 Feb 21;5(4):655-63. doi: 10.1039/b614510h. Epub 2007 Jan 18.

DOI:10.1039/b614510h
PMID:17285174
Abstract

A novel seven-membered lactam formation method has been established by intramolecular ring closure reaction of 4-bromo-(E)-3-[(2-alkylvinyl)carbonylamino]benzo[b]furans under Heck coupling conditions. A number of furo[2,3,4-jk][2]benzazepin-4(3H)-ones, tricyclicbenzo[b]furans, have been prepared by this method and evaluated for their leukotriene B(4) (LTB(4)) receptor and poly(ADP-ribose)polymerase-1 (PARP-1) inhibitory activities.

摘要

通过4-溴-(E)-3-[(2-烷基乙烯基)羰基氨基]苯并[b]呋喃在Heck偶联条件下的分子内环合反应，建立了一种新型的七元内酰胺形成方法。通过该方法制备了许多三环苯并[b]呋喃类的呋喃[2,3,4-jk][2]苯并氮杂䓬-4(3H)-酮，并对它们的白三烯B(4)（LTB(4)）受体和聚（ADP-核糖）聚合酶-1（PARP-1）抑制活性进行了评估。

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