The First Dual ChE/FAAH Inhibitors: New Perspectives for Alzheimer's Disease?

被引：40

作者：

Rampa, Angela ^{[1
]}

Bartolini, Manuela ^{[1
]}

Bisi, Alessandra ^{[1
]}

Belluti, Federica ^{[1
]}

Gobbi, Silvia ^{[1
]}

Andrisano, Vincenza ^{[1
]}

Ligresti, Alessia ^{[2
]}

Di Marzo, Vincenzo ^{[2
]}

机构：

[1] Univ Bologna, Dept Pharmaceut Sci, I-40126 Bologna, Italy

[2] CNR, Inst Biomol Chem, Endocannabinoid Res Grp, I-80078 Pozzuoli, NA, Italy

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2012年 / 3卷 / 03期

关键词：

Alzheimer's disease; drug design; FAAH; AChE; BuChE; carbamate inhibitors; ACID AMIDE HYDROLASE; ACETYLCHOLINESTERASE INHIBITORS; BRAIN; NEUROTOXICITY; CARBAMYLATION; DERIVATIVES; MECHANISM; LIGANDS; SYSTEM; TARGET;

D O I：

10.1021/ml200313p

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The treatment of Alzheimer's disease (AD) still remains an area of significant unmet need, with drugs that only target the symptoms of the disease. Therefore, there is considerable need for disease-modifying therapies. The complex etiology of AD prompts scientists to develop multitarget strategies to combat causes and symptoms. To this aim, we designed, synthesized, and tested four new carbamates as dual cholinesterase-FAAH inhibitors. The dual activity of these compounds could lead to a potentially more effective treatment for the counteraction of AD progression, because they would allow regulation of both ACh and eCB signaling and improve neuronal transmission and/or counteract neuroinflammation.

引用

页码：182 / 186

页数：5

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