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

被引:9
|
作者
Jourdan, Jean-Pierre [1 ]
Since, Marc [1 ]
El Kihel, Laila [1 ]
Lecoutey, Cedric [1 ]
Corvaisier, Sophie [1 ]
Legay, Remi [1 ]
Santos, Jana Sopkova-de Oliveira [1 ]
Cresteil, Thierry [2 ]
Malzert-Freon, Aurelie [1 ]
Rochais, Christophe [1 ]
Dallemagne, Patrick [1 ]
机构
[1] Normandie Univ, Ctr Etud & Rech Medicament Normandie, UNICAEN, CERMN, F-14000 Caen, France
[2] IPSIT IFR141, CIBLOT, F-92290 Chatenay Malabry, France
关键词
Alzheimer's disease; beta-amyloid; antioxidants; MTDL; pyrrolizinones; GLYCOGEN-PHOSPHORYLASE; ALLOSTERIC SITES; STRUCTURAL BASIS; DRUG DISCOVERY; PROTEINS; RECEPTORS; LIGAND; NMR;
D O I
10.1002/cmdc.201700102
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Herein we describe the drug design steps developed to increase the radical scavenging and beta-amyloid aggregation inhibitory activities of a previously described series of benzylide-nephenylpyrrolizinones. 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.
引用
收藏
页码:913 / 916
页数:4
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