4-Cyano-5-(2-thiophenyl)-pyrazoles are high affinity CB1 receptor ligands
Author:
Affiliation:
1. Kosterlitz Centre for Therapeutics
2. Institute of Medical Sciences
3. University of Aberdeen
4. UK
5. Medical Sciences Building
6. University of Toronto
7. Toronto
8. Canada
9. C.N.R.-Istituto di Chimica del Riconoscimento Molecolare
Abstract
Introduction of a 4-CN group on 5-thiophenyl-pyrazoles afforded high affinity cannabinoid ligands having low nM Ki values and moderate CB1 receptor selectivity. Log P and TPSA values suggest that some of the compounds might be peripherally restricted.
Publisher
Royal Society of Chemistry (RSC)
Subject
General Chemical Engineering,General Chemistry
Link
http://pubs.rsc.org/en/content/articlepdf/2015/RA/C4RA17274D
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