Zhang Kena, Tran Christine, Alami Mouad, Hamze Abdallah, Provot Olivier
BioCIS, CNRS-Université Paris-Saclay, 92290 Châtenay-Malabry, France.
Pharmaceuticals (Basel). 2021 Aug 8;14(8):779. doi: 10.3390/ph14080779.
This review concerns the synthesis and biological activities of pyrazino[1,2-]indoles and pyrazino[1,2-]indol-1-ones reported since 1997 and the discovery of biological activity of pyrazinoindole derivatives. In the first part, we first presented the synthetic routes that have been reported from a methodological point of view to access the pyrazinoindole unit according to cyclization reactions using or not using metal catalysts. Then, syntheses and neuropsychiatric, auto-immune, anti-infectious and anti-cancer properties of pyrazinoindoles were detailed. In the second part, we first reported the main accesses to pyrazinoindol-1-one substrates according to Michael reactions, metal-catalyzed and metal-free cyclization reactions. The syntheses and anti-cancer, anti-infectious, anti-allergenic and neuropsychiatric properties of pyrazinoindolones were next described and discussed.
本综述涉及自1997年以来报道的吡嗪并[1,2 - ]吲哚和吡嗪并[1,2 - ]吲哚 - 1 - 酮的合成及生物活性，以及吡嗪吲哚衍生物生物活性的发现。在第一部分，我们首先从方法学角度介绍了已报道的通过使用或不使用金属催化剂的环化反应来获得吡嗪吲哚单元的合成路线。然后，详细阐述了吡嗪吲哚的合成及其神经精神、自身免疫、抗感染和抗癌特性。在第二部分，我们首先根据迈克尔反应、金属催化和无金属环化反应报道了获得吡嗪吲哚 - 1 - 酮底物的主要方法。接下来描述并讨论了吡嗪吲哚酮的合成及其抗癌、抗感染、抗过敏和神经精神特性。
