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Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB2 cannabinoid ligand 1-(2',4'-dichlorophenyl)-6-methyl-N-piperidin-1-yl- 1,4-dihydroindeno[1,2-c]pyrazole-3-carboxamide

Murineddu, Gabriele and Lazzari, Paolo and Ruiu, Stefania and Sanna, Angela and Loriga, Giovanni and Manca, Ilaria and Falzoi, Matteo and Dessì, Cristian and Curzu, Maria Michela and Chelucci, Giorgio Adolfo and Pani, Luca and Pinna, Gérard Aimé (2006) Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB2 cannabinoid ligand 1-(2',4'-dichlorophenyl)-6-methyl-N-piperidin-1-yl- 1,4-dihydroindeno[1,2-c]pyrazole-3-carboxamide. Journal of Medicinal Chemistry, Vol. 49 (25), p. 7502-7512. eISSN 1520-4804. Article.

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DOI: 10.1021/jm060920d

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 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.

Item Type:Article
ID Code:441
Status:Published
Refereed:Yes
Uncontrolled Keywords:Promyelocytic leukemia, carboxamide, piperidine derivatives, HL60 cell line, CB2 cannabinoid receptor, chemical synthesis, structure activity relation, tricyclic compound
Subjects:Area 03 - Scienze chimiche > CHIM/06 Chimica organica
Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Chimica
001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
Publisher:American Chemical Society
eISSN:1520-4804
Deposited On:18 Aug 2009 10:02

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