Synthesis, evaluation against Leishmania amazonensis and cytotoxicity assays in macrophages of sixteen new congeners Morita–Baylis–Hillman adducts

…, NG de Andrade, SMD da Cunha, MR Oliveira…

Index: Silva, Fabio P.L.; De Assis, Priscilla A.C.; Junior, Claudio G.L.; De Andrade, Natalia G.; Da Cunha, Saraghina M.D.; Oliveira, Marcia R.; Vasconcellos, Mario L.A.A. European Journal of Medicinal Chemistry, 2011 , vol. 46, # 9 p. 4295 - 4301

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Citation Number: 13

Abstract

We report the design, synthesis, in vitro evaluation against Leishmania amazonensis (IC50), cytotoxicity assays in macrophages (CC50), and selectivity index (SICC50/IC50) of sixteen new congeners aromatic Morita–Baylis–Hillman adducts 1–16. The 1–16 were prepared in good to excellent yields (58%–97%) from the “one pot” Morita–Baylis–Hillman Reaction between the aldehydes 29–36 and the acrylates 27 or 28 under DABCO as promoter. The ...