Journal
SYNTHESIS-STUTTGART
Volume 47, Issue 6, Pages 817-826Publisher
GEORG THIEME VERLAG KG
DOI: 10.1055/s-0034-1379887
Keywords
cannabinoids; PET imaging; fluorine; Sonogashira reaction; click chemistry
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Funding
- European Commission
- EPSRC National Mass Spectrometry Service Centre
- EPSRC National Mass Spectrometry Service Centre (Swansea, UK)
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Structural modification of the potent conformationally constrained tricyclic pyrazole CB1 ligand NESS0327 was achieved by replacing: (1) the chlorine substituent on the tricycle with a 3-fluoropropyl chain, and (2) the pyrazole 3-{[(piperidino)amino]carbonyl} substituent with a 4-substituted 1,2,3-triazole group obtained by click chemistry from an alkynyl precursor. Among the resulting compounds, two are particularly promising candidates for [F-18]radiolabelling and PET imaging studies of the CB1 receptor, as they displayed K-i CB1=62.5 nM and 42.5 nM, respectively, in the same range as that displayed by rimonabant.
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