Application of the Negishi reaction in the synthesis of thiophene-based lignans analogues with leishmanicidal effects

Lignans represent a well-known group of natural products with anti-protozoal activity. In the literature there are many examples of the anti-parasitic activity of synthetic analogues of lignans containing sulphur bridges. In this work, we have obtained thiophene-based analogues by using a selective and high performance synthetic strategy based on the Negishi cross-coupling reaction. The derivatives were quickly obtained and showed great purity, low toxicity toward a mammalian cell line, and leishmanicidal activity with different potencies.

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Bibliographic Details
Main Authors: Amaral,Mônica F. Z. J., Callejon,Daniel R., Riul,Thalita B., Baruffi,Marcelo D., Toledo,Fabiano T., Lopes,Norberto P., Clososki,Giuliano C.
Format: Digital revista
Language:English
Published: Sociedade Brasileira de Química 2014
Online Access:http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532014001000016
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Summary:Lignans represent a well-known group of natural products with anti-protozoal activity. In the literature there are many examples of the anti-parasitic activity of synthetic analogues of lignans containing sulphur bridges. In this work, we have obtained thiophene-based analogues by using a selective and high performance synthetic strategy based on the Negishi cross-coupling reaction. The derivatives were quickly obtained and showed great purity, low toxicity toward a mammalian cell line, and leishmanicidal activity with different potencies.