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Multi-target 1,4-dihydropyridines showing calcium channel blockade and antioxidant capacity for Alzheimer's disease therapy.
Malek, Rim; Maj, Maciej; Wnorowski, Artur; Józwiak, Krzysztof; Martin, Helene; Iriepa, Isabel; Moraleda, Ignacio; Chabchoub, Fakher; Marco-Contelles, José; Ismaili, Lhassane.
Afiliação
  • Malek R; 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; Laboratory of Applied Chemistry: Heterocycles, Lipids and Polymers, Faculty of Sciences of Sfax, University of Sfax, B
  • Maj M; Department of Biopharmacy, Medical University of Lublin, ul. W. Chodzki 4a, 20-093 Lublin, Poland.
  • Wnorowski A; Department of Biopharmacy, Medical University of Lublin, ul. W. Chodzki 4a, 20-093 Lublin, Poland.
  • Józwiak K; Department of Biopharmacy, Medical University of Lublin, ul. W. Chodzki 4a, 20-093 Lublin, Poland.
  • Martin H; PEPITE EA4267, Laboratoire de Toxicologie Cellulaire, Univ. Bourgogne Franche-Comté, F-25000 Besançon, France.
  • Iriepa I; Departamento de Química Orgánica y Química Inorgánica, Universidad de Alcalá, 28805-Alcalá de Henares, Madrid, Spain; Instituto de Investigación Química Andrés M. del Río (IQAR), Universidad de Alcalá, 28805-Alcalá de Henares, Madrid, Spain.
  • Moraleda I; Departamento de Química Orgánica y Química Inorgánica, Universidad de Alcalá, 28805-Alcalá de Henares, Madrid, Spain.
  • Chabchoub F; Laboratory of Applied Chemistry: Heterocycles, Lipids and Polymers, Faculty of Sciences of Sfax, University of Sfax, B.P 802, 3000 Sfax, Tunisia.
  • Marco-Contelles J; Laboratory of Medicinal Chemistry (IQOG, CSIC), Juan de la Cierva, 3, 28006 Madrid, Spain.
  • Ismaili L; 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 ; 91: 103205, 2019 10.
Article em En | MEDLINE | ID: mdl-31446330
ABSTRACT
In this work we describe the synthesis, Ca+2 channel blockade capacity and antioxidant power of N3,N5-bis(2-(5-methoxy-1H-indol-3-yl)ethyl)-2,6-dimethyl-4-aryl-1,4-dihydropyridine-3,5-dicarboxamides 1-9, a number of multi-target small 1,4-dihydropyridines (DHP), designed by juxtaposition of melatonin and nimodipine. As a result, we have identified antioxidant DHP 7 (Ca2+ channel blockade 55%, and 8.78 Trolox/Equivalents), the most balanced DHP analyzed here, for potential Alzheimer's disease therapy.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Di-Hidropiridinas / Bloqueadores dos Canais de Cálcio / Canais de Cálcio / Cálcio / Doença de Alzheimer / Neuroblastoma / Antioxidantes Tipo de estudo: Prognostic_studies Limite: Humans Idioma: En Ano de publicação: 2019 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Di-Hidropiridinas / Bloqueadores dos Canais de Cálcio / Canais de Cálcio / Cálcio / Doença de Alzheimer / Neuroblastoma / Antioxidantes Tipo de estudo: Prognostic_studies Limite: Humans Idioma: En Ano de publicação: 2019 Tipo de documento: Article