benzofurans and Chronic-Pain

benzofurans has been researched along with Chronic-Pain* in 1 studies

Other Studies

1 other study(ies) available for benzofurans and Chronic-Pain

Article	Year
Conformationally constrained analogs of BAY 59-3074 as novel cannabinoid receptor ligands. Bioorganic & medicinal chemistry letters, 2011, Oct-01, Volume: 21, Issue:19 To obtain information on the pharmacophoric requirements of the CB1/CB2 partial agonist BAY 59-3074 we have synthesized a series of new conformationally constrained dibenzofuran (4a-d) and dibenzopyran analogs (5). All constrained analogs exhibited reduced binding affinity at both cannabinoid receptor subtypes, suggesting that planar conformations of these ligands are less favored by both receptors. We also found that 4c, 4d, and 5 exhibited 3- to 12-fold selectivity for hCB2 over rCB1 receptors and may serve as new chemotypes for the development of CB2-selective cannabinergics. Topics: Alkanesulfonates; Analgesics; Animals; Benzofurans; Benzopyrans; Chronic Pain; Computer Simulation; Drug Design; Drug Evaluation, Preclinical; Humans; Ligands; Mice; Molecular Conformation; Molecular Targeted Therapy; Neuralgia; Nitriles; Protein Binding; Radioligand Assay; Receptor, Cannabinoid, CB1; Receptor, Cannabinoid, CB2; Software; Structure-Activity Relationship; Substrate Specificity	2011

Article

Year

Conformationally constrained analogs of BAY 59-3074 as novel cannabinoid receptor ligands.

Bioorganic & medicinal chemistry letters, 2011, Oct-01, Volume: 21, Issue:19

To obtain information on the pharmacophoric requirements of the CB1/CB2 partial agonist BAY 59-3074 we have synthesized a series of new conformationally constrained dibenzofuran (4a-d) and dibenzopyran analogs (5). All constrained analogs exhibited reduced binding affinity at both cannabinoid receptor subtypes, suggesting that planar conformations of these ligands are less favored by both receptors. We also found that 4c, 4d, and 5 exhibited 3- to 12-fold selectivity for hCB2 over rCB1 receptors and may serve as new chemotypes for the development of CB2-selective cannabinergics.

Topics: Alkanesulfonates; Analgesics; Animals; Benzofurans; Benzopyrans; Chronic Pain; Computer Simulation; Drug Design; Drug Evaluation, Preclinical; Humans; Ligands; Mice; Molecular Conformation; Molecular Targeted Therapy; Neuralgia; Nitriles; Protein Binding; Radioligand Assay; Receptor, Cannabinoid, CB1; Receptor, Cannabinoid, CB2; Software; Structure-Activity Relationship; Substrate Specificity

2011