Direct synthesis of C3-mono-functionalized oxindoles from N-unprotected 2-oxindole and their antileishmanial activity |
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| Institution: | 1. Instituto de Ciências Ambientais, Químicas e Farmacêuticas, Universidade Federal de São Paulo, São Paulo, Brazil;2. Laboratório de Patologia de Moléstias Infecciosas (LIM-50), Departamento de Patologia, Faculdade de Medicina, Universidade de São Paulo, São Paulo, Brazil;3. Departamento de Botânica, Instituto de Biociências, Universidade de São Paulo, São Paulo, Brazil |
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| Abstract: | A novel approach for the synthesis of unprecedented C3-mono-functionalized indolin-2-ones is reported, starting from 2-oxindole and chalcones. The reactions proceed regioselectively under mild conditions, without di- and tri-alkylated side products. The new compounds have been evaluated in vitro for their antiproliferative effects against the protozoan Leishmania infantum. Interestingly, they appear able to kill L. infantum promastigotes and amastigotes, without significant cytotoxic effects. |
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| Keywords: | Oxindoles Michael addition Cyclization Diastereoselectivity Leishmanicidal activity |
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