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Receptor Affinity and Phosphodiesterases 4b and 10a Activity of Octahydro- and 6,7-Dimethoxy-3,4-Dihydro- Isoquinolin-2 (1h) -Yl-Alkyl Derivatives of Imidazo- and Pyrimidino[2,1-F]purines

Zagórska, A.; Gryzło, B.; Satała, G.; Bojarski, A.J.; Głuch-Lutwin, M.; Mordyl, B.; Kazek, G.; Pawłowski, M.

Acta Poloniae Pharmaceutica 73(2): 369-377

2016

ISSN/ISBN: 0001-6837
PMID: 27180429
Document Number: 690097
A series of octahydro- and 6,7-dimethoxy-3,4-dihydro- isoquinolin-2(1H)-yl-alkyl derivatives of imidazo- and pyrimidino[2,1-f]purines were synthesized and biologically evaluated in in vitro competition binding experiments for serotonin 5-HT(1A), 5-HT(6), 5-HT(7), and dopamine D2 receptors and inhibitory potencies for phosphodiesterases - PDE4B1 and PDE10A. The structure-activity relationships allowed to determine the structural features responsible for receptor and enzyme activity. Compound 5 (8-(4-(6,7-dimethoxy-3,4-dihydroiso- quinolin-2(1H)butyl)1,3-dimethyl-H-imidazo[2,1-f]purine-2,4(3H,8H)-dione) could be regarded as promising structure for further modification and detailed mechanistic study for obtained hybrid ligands.

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