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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.
Nettekoven M1, Fingerle J, Grether U, Grüner S, Kimbara A, Püllmann B, Rogers-Evans M, Röver S, Schuler F, Schulz-Gasch T, Ullmer C.
1F. Hoffmann-La Roche Ltd, Pharma Research & Early Development, Medicinal Chemistry, Grenzacher Str. 124, 4070 Basel, Switzerland. email@example.com
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 ß-arrestin data which will support the insight into their relevance for the in vivo situation.