New analogues (2a-p) of the previously reported CB 2 ligands 6-methyl- and 6-chloro-1-(2′,4′-dichlorophenyl)-N-piperidin-1-yl-1, 4-dihydroindeno[1,2-c]pyrazole-3-carboxamides (1a,b) have been synthesized and evaluated for cannabinoid receptor affinity. One example, 1-(2′,4′- dichlorophenyl)-6-methyl-N-cyclohexyilamine-1,4-dihydroindeno[1,2-c] pyrazole-3-carboxamide (2a) was shown to have single digit nanomolar affinity for cannabinoid CB 2 receptors. Furthermore, compounds 2a and 2b, as well as lead structures 1a,b, were also shown to be agonist in an in vitro model based on human promyelocytic leukemia HL-60 cells. © 2006 American Chemical Society.
Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB 2 cannabinoid ligand 1-(2′, 4′-dichlorophenyl)-6-methyl-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c] pyrazole-3-carboxamide / Murineddu, G., Lazzari, P., Ruiu, S., Sanna, A., Loriga, G., Manca, I., Falzoi, M., Dessi, C., Curzu, M.M., Chelucci, G., Pani, L., Pinna, G.A.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 49:25(2006), pp. 7502-7512. [10.1021/jm060920d]
Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB 2 cannabinoid ligand 1-(2′, 4′-dichlorophenyl)-6-methyl-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c] pyrazole-3-carboxamide
Lazzari P.;Pani L.;
2006
Abstract
New analogues (2a-p) of the previously reported CB 2 ligands 6-methyl- and 6-chloro-1-(2′,4′-dichlorophenyl)-N-piperidin-1-yl-1, 4-dihydroindeno[1,2-c]pyrazole-3-carboxamides (1a,b) have been synthesized and evaluated for cannabinoid receptor affinity. One example, 1-(2′,4′- dichlorophenyl)-6-methyl-N-cyclohexyilamine-1,4-dihydroindeno[1,2-c] pyrazole-3-carboxamide (2a) was shown to have single digit nanomolar affinity for cannabinoid CB 2 receptors. Furthermore, compounds 2a and 2b, as well as lead structures 1a,b, were also shown to be agonist in an in vitro model based on human promyelocytic leukemia HL-60 cells. © 2006 American Chemical Society.
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