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

来源：

CHEMMEDCHEM | 2017年 / 12卷 / 12期

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

页码：913 / 916

页数：4

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