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Synthesis and SAR study of novel tricyclic pyrazoles as potent phosphodiesterase 10A inhibitors

Dore, Antonio and Asproni, Battistina and Scampuddu, Alessia and Pinna, Gérard Aimé and Tornby Christoffersen, Claus and Langgàrd, Morten and Kehler, Jan (2014) Synthesis and SAR study of novel tricyclic pyrazoles as potent phosphodiesterase 10A inhibitors. European Journal of Medicinal Chemistry, Vol. 84 , p. 181-193. ISSN 0223-5234. Article.

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DOI: 10.1016/j.ejmech.2014.07.020


Novel pyrazolo[5,1-f][1,6]naphthyridines, pyrazolo[5,1-a][2,6]naphthyridines, pyrazolo[5,1-a][2,7]naphthyridines and pyrazolo[5,1-a]isoquinolines phenylimidazole/benzimidazole ethylene-linked were designed and synthesized for PDE10A interaction. An AgOTf and proline-cocatalyzed multicomponent methodology based on use of o-alkynylaldehydes, tosylhydrazide and ketones was developed and proved to be a convenient route for assembly of most of the novel tricyclic pyrazoles synthesized. Pyrazolo[5,1-f][1,6]naphthyridine 43 and 59, pyrazolo[5,1-a][2,6]naphthyridine 66, and pyrazolo[5,1-a][2,7]naphthyridine 42 showed the highest affinity for PDE10A enzyme (IC50 = 40, 42, 40, 55 nM, respectively).

Item Type:Article
ID Code:9997
Uncontrolled Keywords:Tricyclic pyrazoles, PDE10A inhibition, structure–activity relationships
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01-a Nuovi Dipartimenti dal 2012 > Chimica e Farmacia
Publisher:Elsevier Masson
Deposited On:01 Aug 2014 09:30

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