1334831-80-9Relevant academic research and scientific papers
Electrochemical and computational studies, in protic medium, of Morita-Baylis-Hillman adducts and correlation with leishmanicidal activity
De Paiva, Yen G.,Pinho Júnior, Waldomiro,De Souza, Antonio A.,Costa, Cícero O.,Silva, Fábio P.L.,Lima-Junior, Cláudio G.,Vasconcellos, Mario L.A.A.,Goulart, Marília O.F.
, p. 557 - 563 (2014)
Enzymatic bioreduction of nitro groups plays an important role on the activity of biologically active nitroaromatic compounds. Electrochemical methods are useful tools to simulate in vivo metabolic processes. This work presents electrochemical studies, in
Correlation between electrochemical and theoretical studies on the leishmanicidal activity of twelve Morita-Baylis-Hillman adducts
De Paiva, Yen G.,De Souza, Anto?nio A.,Lima-Junior, Claudio G.,Silva, Fa?bio P. L.,Filho, Edilson B. A.,De Vasconcelos, Camila C.,De Abreu, Fabiane C.,Goulart, Mari?lia O. F.,Vasconcellos, Ma?rio L. A. A.
scheme or table, p. 894 - 904 (2012/06/18)
Enzymatic bioreduction of nitro groups plays an important role on the activity of biologically active nitroaromatic compounds. Electrochemical methods are useful tools to simulate in vivo metabolic processes. This work presents electrochemical studies in
Synthesis, evaluation against Leishmania amazonensis and cytotoxicity assays in macrophages of sixteen new congeners Morita-Baylis-Hillman adducts
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.
experimental part, p. 4295 - 4301 (2011/11/13)
We report the design, synthesis, in vitro evaluation against Leishmania amazonensis (IC50), cytotoxicity assays in macrophages (CC 50), 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 MBHA 2-[Hydroxy(2-nitrophenyl)propyl] propanoate (1, IC50 = 7.52 μg/mL or 28.38 μM; CC50 = 35.77 μg/mL or 134.98 μM; SI = 4.75) and 2-[Hydroxy(2-nitrophenyl) hydroxyethyl] propanoate (9, IC50 = 5.48 μg/mL or 20.52 μM; CC50 = 29.81 μg/mL or 111.64c μM and, SI = 5.43) were the most effective and safe evaluated compounds.
