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• W2046702761 abstract "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)." @default.
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• W2046702761 date "2014-09-01" @default.
• W2046702761 modified "2023-10-15" @default.
• W2046702761 title "Synthesis and SAR study of novel tricyclic pyrazoles as potent phosphodiesterase 10A inhibitors" @default.
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• W2046702761 doi "https://doi.org/10.1016/j.ejmech.2014.07.020" @default.
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