Discovery of 4-hydroxy-1,6-naphthyridine-3-carbonitrile derivatives as novel PDE10A inhibitors.
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Bauer U, Giordanetto F, Bauer M, O'Mahony G, Johansson KE, Knecht W, Hartleib-Geschwindner J, Carlsson ET, Enroth C
Discovery of 4-hydroxy-1,6-naphthyridine-3-carbonitrile derivatives as novel PDE10A inhibitors.
Bioorg Med Chem Lett. 2012 Mar 1;22(5):1944-8. doi: 10.1016/j.bmcl.2012.01.046. Epub 2012 Jan 26.
- PubMed ID
- 22321214 [ View in PubMed]
- Abstract
A series of 1,6-naphthyridine-based compounds was synthesized as potent phosphodiesterase 10A (PDE10A) inhibitors. Structure-based chemical modifications of the discovered chemotype served to further improve potency and selectivity over DHODH, laying the foundation for future optimization efforts.
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) 4,5-bis(4-methoxyphenyl)-2-thiophen-2-yl-1H-imidazole cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A IC 50 (nM) 35 N/A N/A Details Papaverine cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A IC 50 (nM) 36 N/A N/A Details