-transparent.png){kind=logo}
A large series of 2-aryl-2,5-dihydropyridazino[4,3-b]indol-3(3H)ones (PIs) carrying properly selected substituents at the indole and N2-phenyl rings was prepared and tested as central benzodiazepine receptor (BZR) ligands and potential (anti)convulsant agents. Stereoelectronic requirements for high receptor affinity were detected by means of 2-D and 3-D QSAR analyses. BZR affinities and pharmacological profiles of the compounds were examined in comparison with some other pyridazinoindolones recently described by us and with pyrazoloquinoline (PQ) analogues. An anticonvulsant activity greater than PQs was generally observed for PIs. Notably, in the test of audiogenically induced seizures, one compound showed a potency comparable to that of diazepam.
F Palluotto, and
A Carotti, and
G Casini, and
F Campagna, and
G Genchi, and
M Rizzo, and
G B De Sarro
May 2014,
European journal of medicinal chemistry,
F Palluotto, and
A Carotti, and
G Casini, and
F Campagna, and
G Genchi, and
M Rizzo, and
G B De Sarro
January 1992,
Journal of medicinal chemistry,
F Palluotto, and
A Carotti, and
G Casini, and
F Campagna, and
G Genchi, and
M Rizzo, and
G B De Sarro
April 2003,
The Journal of organic chemistry,
F Palluotto, and
A Carotti, and
G Casini, and
F Campagna, and
G Genchi, and
M Rizzo, and
G B De Sarro
May 2023,
Organic & biomolecular chemistry,
F Palluotto, and
A Carotti, and
G Casini, and
F Campagna, and
G Genchi, and
M Rizzo, and
G B De Sarro
February 2024,
The Journal of organic chemistry,
F Palluotto, and
A Carotti, and
G Casini, and
F Campagna, and
G Genchi, and
M Rizzo, and
G B De Sarro
January 1988,
Journal of medicinal chemistry,
F Palluotto, and
A Carotti, and
G Casini, and
F Campagna, and
G Genchi, and
M Rizzo, and
G B De Sarro
February 2001,
Bioorganic & medicinal chemistry,
F Palluotto, and
A Carotti, and
G Casini, and
F Campagna, and
G Genchi, and
M Rizzo, and
G B De Sarro
July 2004,
Bioorganic & medicinal chemistry letters,
F Palluotto, and
A Carotti, and
G Casini, and
F Campagna, and
G Genchi, and
M Rizzo, and
G B De Sarro
September 1993,
Journal of medicinal chemistry,
F Palluotto, and
A Carotti, and
G Casini, and
F Campagna, and
G Genchi, and
M Rizzo, and
G B De Sarro
March 2020,
Angewandte Chemie (International ed. in English),
