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Synthesis, antioxidant and Aß anti-aggregation properties of new ferulic, caffeic and lipoic acid derivatives obtained by the Ugi four-component reaction.
Benchekroun, Mohamed; Pachón-Angona, Irene; Luzet, Vincent; Martin, Helene; Oset-Gasque, María-Jesús; Marco-Contelles, José; Ismaili, Lhassane.
Afiliação
  • Benchekroun M; Laboratoire Neurosciences intégratives et cliniques EA 481, Pôle de Chimie Organique et Thérapeutique, Univ. Bourgogne Franche-Comté, UFR Santé, 19, rue Ambroise Paré, F-25000 Besançon, France.
  • Pachón-Angona I; Laboratoire Neurosciences intégratives et cliniques EA 481, Pôle de Chimie Organique et Thérapeutique, Univ. Bourgogne Franche-Comté, UFR Santé, 19, rue Ambroise Paré, F-25000 Besançon, France.
  • Luzet V; Laboratoire Neurosciences intégratives et cliniques EA 481, Pôle de Chimie Organique et Thérapeutique, Univ. Bourgogne Franche-Comté, UFR Santé, 19, rue Ambroise Paré, F-25000 Besançon, France.
  • Martin H; PEPITE EA4267, Laboratoire de Toxicologie Cellulaire, Univ. Bourgogne Franche-Comté, F-25000 Besançon, France.
  • Oset-Gasque MJ; Faculty of Pharmacy, Department of Biochemistry and Molecular Biology, Complutense University, 28040-Madrid, Spain.
  • Marco-Contelles J; Laboratory of Medicinal Chemistry (IQOG, CSIC), Juan de la Cierva 3, 28006 Madrid, Spain.
  • Ismaili L; Laboratoire Neurosciences intégratives et cliniques EA 481, Pôle de Chimie Organique et Thérapeutique, Univ. Bourgogne Franche-Comté, UFR Santé, 19, rue Ambroise Paré, F-25000 Besançon, France. Electronic address: lhassane.ismaili@univ-fcomte.fr.
Bioorg Chem ; 85: 221-228, 2019 04.
Article em En | MEDLINE | ID: mdl-30640071
We report herein the synthesis antioxidant and Aß anti-aggregation capacity of (E)-N-benzyl-N-[2-(benzylamino)-2-oxoethyl]-3-(aryl)acrylamides and related (R)-N-benzyl-N-(2-(benzylamino)-2-oxoethyl)-5-(1,2-dithiolan-3-yl)pentanamides 1-12. These compounds have been obtained, via Ugi four-component reaction, from modest to good yields. Their antioxidant analysis, using the DPPH and ORAC assays, allowed us to identify compounds 8 and 9, as potent antioxidant agents, showing also strong Aß1-40 self-aggregation inhibition, two biological properties of interest in pathologies linked to the oxidative stress, such as Alzheimer's disease.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Ácidos Cafeicos / Sequestradores de Radicais Livres / Ácido Tióctico / Ácidos Cumáricos / Multimerização Proteica Limite: Humans Idioma: En Ano de publicação: 2019 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Ácidos Cafeicos / Sequestradores de Radicais Livres / Ácido Tióctico / Ácidos Cumáricos / Multimerização Proteica Limite: Humans Idioma: En Ano de publicação: 2019 Tipo de documento: Article