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Issue 18, 2015
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4-Cyano-5-(2-thiophenyl)-pyrazoles are high affinity CB1 receptor ligands

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Abstract

Pyrazoles bearing a 5-thiophenyl and a 4-cyano group were synthesised and tested for their affinity to the cannabinoid CB1 receptor showing in many cases single digit nanomolar Ki values and moderate to good selectivity towards the CB2 receptor. Some of these pyrazole ligands, such as 8g, displayed relatively low lipophilicity (experimental log P < 4) and high calculated Topological Polar Surface Area (TPSA) (>90) suggesting that these compounds may behave as peripherally restricted CB1 ligands. Furthermore, 2-fluoroethyl carboxamides 8d, 8h and 8l are interesting candidates for further development into PET tracers.

Graphical abstract: 4-Cyano-5-(2-thiophenyl)-pyrazoles are high affinity CB1 receptor ligands

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Supplementary files

Article information


Submitted
30 Dec 2014
Accepted
19 Jan 2015
First published
21 Jan 2015

RSC Adv., 2015,5, 13692-13701
Article type
Paper
Author version available

4-Cyano-5-(2-thiophenyl)-pyrazoles are high affinity CB1 receptor ligands

S. Altomonte, G. L. Baillie, R. A. Ross and M. Zanda, RSC Adv., 2015, 5, 13692
DOI: 10.1039/C4RA17274D

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