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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.

thiophene; leishmanicidal; Negishi reaction; cross-coupling; green chemistry


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