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

Sansook, Supojjanee, Tuo, Wei, Bollier, Mélanie, Barczyk, Amélie, Dezitter, Xavier, Klupsch, Fredérique, Leleu-Chavain, Natascha, Farce, Amaury, Tizzard, Graham J, Coles, Simon J, Spencer, John and Millet, Regis (2017) Synthesis and biological evaluation of ferrocene-based cannabinoid receptor 2 ligands. Future Medicinal Chemistry. ISSN 1756-8919 (Accepted)

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Abstract

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

Item Type: Article
Schools and Departments: School of Life Sciences > Chemistry
Subjects: Q Science > QD Chemistry > QD0241 Organic chemistry
Q Science > QD Chemistry > QD0241 Organic chemistry > QD0415 Biochemistry
Depositing User: John Spencer
Date Deposited: 18 Dec 2017 09:45
Last Modified: 18 Dec 2017 09:45
URI: http://sro.sussex.ac.uk/id/eprint/72224

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