Synthesis and Biological Activities of Pyrazino[1,2-a]indole and Pyrazino[1,2-a]indol-1-one Derivatives

This review concerns the synthesis and biological activities of pyrazino[1,2-a]indoles and pyrazino[1,2-a]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.

Automated summary

This review summarizes the synthesis and biological activities of pyrazino[1,2-a]indoles and pyrazino[1,2-a]indol-1-ones reported since 1997, as well as the discovery of biological activity of pyrazinoindole derivatives. The review discusses synthetic routes to access the pyrazinoindole unit and the properties of pyrazinoindoles, including neuropsychiatric, auto-immune, anti-infectious, and anti-cancer properties. It also covers the main accesses to pyrazinoindol-1-one substrates and the properties of pyrazinoindolones, such as anti-cancer, anti-infectious, anti-allergenic, and neuropsychiatric properties.