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2-Aryl-2,5-dihydropyridazino[4,3-b]lindol-3(3H)-ones: Novel rigid planar benzodiazepine receptor ligands |
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| Authors: | F Campagna A Carotti G Casini F Palluotto G Genchi and G B De Sarro |
| Institution: | a Dipartimento Farmacochimico, via Orabona 4, University of Bari, 70126 Bari, Italy b Dipartimento di Scienze Animali, Vegetali e dell'Ambiente, University of Molise, Campobasso, Italy c Dipartimento di Medicina Sperimentale e Clinica, University of Reggio Calabria, Catanzaro, Italy |
| Abstract: | A series of 2-aryl-2,5-dihydropyridazino4,3-b]indol-3(3H)-ones 5 were prepared and evaluated for their ability to inhibit radioligand binding to BZR, and to prevent sound and pentylenetetrazole (PTZ) induced seizures in mice. The biological and pharmacological results are discussed in the light of some recently proposed pharmacophore models and compared through molecular orbital and molecular modeling studies to those obtained from the close pyrazoloquinoline analogs 6. |
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