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00925njm 22002777a 4500 dc Murineddu, Gabriele author Deligia, Francesco author Ragusa, Giulio author García Toscano, Laura author Gómez Cañas, María author Asproni, Battistina author Satta, Valentina author Cichero, Elena author Pazos, Ruth author Fossa, Paola author Loriga, Giovanni author Fernández Ruiz, José Javier author Pinna, Gerard A. author 2018-01 A series of sulfenamide and sulfonamide derivatives was synthesized and evaluated for the affinity at CB1 and CB2 receptors. The N-bornyl-S-(5,6-di-p-tolylpyridazin-3-yl)-sulfenamide, compound 11, displayed good affinity and high selectivity for CB1 receptors (Ki values of 44.6 nM for CB1 receptors and >40 μM for CB2 receptors, respectively). The N-isopinocampheyl-sulfenamide 12 and its sulfonamide analogue 22 showed similar selectivity for CB1 receptors with Ki values of 75.5 and 73.2 nM, respectively. These novel compounds behave as antagonists/inverse agonists at CB1 receptor in the [35S]-GTPγS binding assays, and none showed adequate predictive blood–brain barrier permeation, exhibiting low estimated LD50. However, testing compound 12 in a supraspinal analgesic test (hot-plate) revealed that it was as effective as the classic CB1 receptor antagonist rimonabant, in reversing the analgesic effect of a cannabinoid agonist. Murineddu G, Deligia F, Ragusa G, García-Toscano L, Gómez-Cañas M, Asproni B, et al. Novel sulfenamides and sulfonamides based on pyridazinone and pyridazine scaffolds as CB1 receptor ligand antagonists. Bioorganic & Medicinal Chemistry 2018;26:295–307. https://doi.org/10.1016/j.bmc.2017.11.051 0968-0896 10.1016/j.bmc.2017.11.051 https://hdl.handle.net/20.500.14352/131205 https://doi.org/10.1016/J.BMC.2017.11.051 https://www.sciencedirect.com/science/article/pii/S0968089617318667?via%3Dihub Novel sulfenamides and sulfonamides based on pyridazinone and pyridazine scaffolds as CB1 receptor ligand antagonists