Bioorganic and Medicinal Chemistry Letters p. 2574 - 2579 (2008)
Update date:2022-08-04
Topics:
Verbist, Bie M.P.
De Cleyn, Michel A.J.
Surkyn, Michel
Fraiponts, Erwin
Aerssens, Jeroen
Nijsen, Marjoleen J.M.A.
Gijsen, Harrie J.M.
A novel series of benzimidazole CB2-receptor agonists was synthesized and the structure-activity relationship explored. The results showed agonistic activities with an EC50 up to 0.5 nM and excellent selectivity (>4000-fold) over the CB1 receptor. The size of the substituent on the 2-position determined the level of agonism, ranging from inverse agonism to partial agonism to full agonism, which was more pronounced for the rat CB2 receptor. A wide variation of sulfonyl substituents at the benzimidazole 5-position was tolerated, which was used to optimize the drug-like properties. This resulted into lead compound 14j that can be used to investigate the potential of a selective, peripherically acting CB2 agonist. The in vitro profile of key compounds is displayed using pie bar charts (VlaaiVis).
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(2008)