Novel anellated pyrazoloquinolin-3-ones: synthesis and in vitro BZR activity

…, S Dall'Acqua, E Maciocco, MP Mascia, MG Pisu…

Index: Ferlin, Maria Grazia; Chiarelotto, Gianfranco; Dall'Acqua, Stefano; MacIocco, Elisabetta; Mascia, Maria Paola; Pisu, Maria Giuseppina; Biggio, Giovanni Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 10 p. 3531 - 3541

Full Text: HTML

Citation Number: 25

Abstract

A series of pyrazolo [4, 3-c] pyrrolo [3, 2-f] quinolin-3-one derivatives 6, 7a–c, 8a, b, 9a, b and 10–12 were synthesized as modified pyrazoloquinolinone analogs (PQs) and evaluated for their ability to inhibit radioligand to central and peripheral benzodiazepine receptors (BZRs) and their effect on GABAA α1β2γ2L receptors expressed in Xenopus laevis oocytes. Multistep synthesis starting from 5-nitroindole, via the Gould–Jacobs reaction to the ...