Skip to main page content
Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
, 18 (8), 2574-9

5-Sulfonyl-benzimidazoles as Selective CB2 Agonists

Affiliations

5-Sulfonyl-benzimidazoles as Selective CB2 Agonists

Bie M P Verbist et al. Bioorg Med Chem Lett.

Abstract

A novel series of benzimidazole CB2-receptor agonists was synthesized and the structure-activity relationship explored. The results showed agonistic activities with an EC(50) 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).

Similar articles

See all similar articles

Cited by 2 PubMed Central articles

LinkOut - more resources

Feedback