Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2013 Mar 1;23(5):1177-81. doi: 10.1016/j.bmcl.2013.01.044. Epub 2013 Jan 23.

Highly potent and selective cannabinoid receptor 2 agonists: initial hit optimization of an adamantyl hit series identified from high-through-put screening.

Author information

1
F. Hoffmann-La Roche Ltd, Pharma Research & Early Development, Medicinal Chemistry, Grenzacher Str. 124, 4070 Basel, Switzerland. matthias.nettekoven@roche.com

Abstract

A series of highly potent & selective adamantane derived CB2 agonists was identified in a high-throughput screen. A SAR was established and physicochemical properties were significantly improved. This was accompanied by potency of the compounds on the Q63R variant and varying β-arrestin data which will support the insight into their relevance for the in vivo situation.

PMID:
23380378
DOI:
10.1016/j.bmcl.2013.01.044
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center