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

Pub. Date : 2014 Sep 12

PMID : 25016376






2 Functional Relationships(s)
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1 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. pyrazolo(5,1-f)(1,6)naphthyridine phosphodiesterase 10A Homo sapiens
2 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). pyrazolo(5,1-f)(1,6)naphthyridine phosphodiesterase 10A Homo sapiens