Synthesis and biological evaluation of ferrocene-based cannabinoid receptor 2 ligands

被引：8

作者：

Sansook, Supojjanee ^{[1
]}

Tuo, Wei ^{[2
]}

Bollier, Melanie ^{[2
]}

Barczyk, Amelie ^{[2
]}

Dezitter, Xavier ^{[2
]}

Klupsch, Frederique ^{[2
]}

Leleu-Chavain, Natascha ^{[2
]}

Farce, Amaury ^{[2
]}

Tizzard, Graham J. ^{[3
]}

Coles, Simon J. ^{[3
]}

Spencer, John ^{[1
]}

Millet, Regis ^{[2
]}

机构：

[1] Univ Sussex, Sch Life Sci, Dept Chem, Brighton BN1 9QJ, E Sussex, England

[2] Univ Lille, INSERM, CHU Lille, U995,LIRIC, F-59000 Lille, France

[3] Univ Southampton, Sch Chem, UK Natl Crystallog Serv, Southampton SO17 1BJ, Hants, England

来源：

FUTURE MEDICINAL CHEMISTRY | 2018年 / 10卷 / 06期

关键词：

cannabinoids; FAAH; ferrocene; isoxazole; ACID AMIDE HYDROLASE; TRANSFECTED CELLS; FAAH INHIBITORS; CB2; AGONISTS; ANANDAMIDE; AM630; TRANSPORT; MOIETY; BRAIN;

D O I：

10.4155/fmc-2017-0200

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Ferrocene analogs of known fatty acid amide hydrolase inhibitors and CB2 ligands have been synthesized and characterized spectroscopically and crystallographically. The resulting bio-organometallic isoxazoles were assayed for their effects on CB1 and CB2 receptors as well as on fatty acid amide hydrolase. None had any fatty acid amide hydrolase activity but compound 3, 5-(2-(pentyloxy)phenyl)-N-ferrocenylisoxazole-3carboxamide, was found to be a potent CB2 ligand (K-i = 32.5 nM).

引用

页码：631 / 638

页数：8

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