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

This review concerns the synthesis and biological activities of pyrazino[1,2-<i>a</i>]indoles and pyrazino[1,2-<i>a</i>]indol-1-ones reported since 1997 and the discovery of biological activity of pyrazinoindole derivatives. In the first part, we first presented the synthetic...

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Main Authors: Kena Zhang (Author), Christine Tran (Author), Mouad Alami (Author), Abdallah Hamze (Author), Olivier Provot (Author)
Format: Book
Published: MDPI AG, 2021-08-01T00:00:00Z.
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Summary:This review concerns the synthesis and biological activities of pyrazino[1,2-<i>a</i>]indoles and pyrazino[1,2-<i>a</i>]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.
Item Description:10.3390/ph14080779
1424-8247