Literature DB >> 28342294

Benzylphenylpyrrolizinones with Anti-amyloid and Radical Scavenging Effects, Potentially Useful in Alzheimer's Disease Treatment.

Jean-Pierre Jourdan1, Marc Since1, Laïla El Kihel1, Cédric Lecoutey1, Sophie Corvaisier1, Rémi Legay1, Jana Sopková-de Oliveira Santos1, Thierry Cresteil2, Aurélie Malzert-Fréon1, Christophe Rochais1, Patrick Dallemagne1.   

Abstract

Herein we describe the drug design steps developed to increase the radical scavenging and β-amyloid aggregation inhibitory activities of a previously described series of benzylidenephenylpyrrolizinones. Among the newly synthesized derivatives, some benzylphenylpyrrolizinones exhibited interesting results in regard to those activities. Initial druggability parameters were measured, and suggest these compounds as a suitable starting point for potential alternatives in treating Alzheimer's disease.
© 2017 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

Entities:  

Keywords:  Alzheimer′s disease; MTDL; antioxidants; pyrrolizinones; β-amyloid

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Year:  2017        PMID: 28342294     DOI: 10.1002/cmdc.201700102

Source DB:  PubMed          Journal:  ChemMedChem        ISSN: 1860-7179            Impact factor:   3.466


  1 in total

1.  New 8-Nitroquinolinone Derivative Displaying Submicromolar in Vitro Activities against Both Trypanosoma brucei and cruzi.

Authors:  Julien Pedron; Clotilde Boudot; Jean-Yves Brossas; Emilie Pinault; Sandra Bourgeade-Delmas; Alix Sournia-Saquet; Elisa Boutet-Robinet; Alexandre Destere; Antoine Tronnet; Justine Bergé; Colin Bonduelle; Céline Deraeve; Geneviève Pratviel; Jean-Luc Stigliani; Luc Paris; Dominique Mazier; Sophie Corvaisier; Marc Since; Aurélie Malzert-Fréon; Susan Wyllie; Rachel Milne; Alan H Fairlamb; Alexis Valentin; Bertrand Courtioux; Pierre Verhaeghe
Journal:  ACS Med Chem Lett       Date:  2020-02-06       Impact factor: 4.345

  1 in total

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