Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB2 cannabinoid ligand 1-(2', 4'-dichlorophenyl)-6-methyl-N- …

G Murineddu, P Lazzari, S Ruiu, A Sanna…

Index: Murineddu, Gabriele; Lazzari, Paolo; Ruiu, Stefania; Sanna, Angela; Loriga, Giovanni; Manca, Ilaria; Falzoi, Matteo; Dessi, Christian; Curzu, Maria M.; Chelucci, Giorgio; Pani, Luca; Pinna, Gerard A. Journal of Medicinal Chemistry, 2006 , vol. 49, # 25 p. 7502 - 7512

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Citation Number: 61

Abstract

New analogues (2a-p) of the previously reported CB2 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 CB2 ...