-transparent.png){kind=logo}
A series of 1-aryl-3,5-dimethyl-4,5-dihydro-1H-pyrazolo[4,5-c]quinolin-4-ones (2a-e) and 1-aryl-3-methyl-1H-pyrazolo[4,5-c]quinolines (3-7a-e) bearing different substituents at position 4 were prepared and tested for their ability to displace specific [3H]flunitrazepam binding from bovine brain membranes. The 5-N-methyl derivatives 2a-c,e were the compounds that bound with the highest affinity within this class. The replacement of the carbonyl group with other substituents and the resulting aromatization of the pyridine moiety greatly decreased the binding affinity. From a Lineweaver-Burk analysis on the most active compound 2b, it appears that the inhibition is a competitive one.
F Melani, and
L Cecchi, and
G Palazzino, and
G Filacchioni, and
C Martini, and
E Pennacchi, and
A Lucacchini
January 1993,
Farmaco (Societa chimica italiana : 1989),
F Melani, and
L Cecchi, and
G Palazzino, and
G Filacchioni, and
C Martini, and
E Pennacchi, and
A Lucacchini
December 1993,
Farmaco (Societa chimica italiana : 1989),
F Melani, and
L Cecchi, and
G Palazzino, and
G Filacchioni, and
C Martini, and
E Pennacchi, and
A Lucacchini
July 1989,
Research communications in chemical pathology and pharmacology,
F Melani, and
L Cecchi, and
G Palazzino, and
G Filacchioni, and
C Martini, and
E Pennacchi, and
A Lucacchini
June 2002,
Die Pharmazie,
F Melani, and
L Cecchi, and
G Palazzino, and
G Filacchioni, and
C Martini, and
E Pennacchi, and
A Lucacchini
June 1994,
Drug design and discovery,
F Melani, and
L Cecchi, and
G Palazzino, and
G Filacchioni, and
C Martini, and
E Pennacchi, and
A Lucacchini
December 1997,
Archiv der Pharmazie,
F Melani, and
L Cecchi, and
G Palazzino, and
G Filacchioni, and
C Martini, and
E Pennacchi, and
A Lucacchini
July 1996,
Journal of medicinal chemistry,
F Melani, and
L Cecchi, and
G Palazzino, and
G Filacchioni, and
C Martini, and
E Pennacchi, and
A Lucacchini
September 1993,
Journal of pharmaceutical sciences,
F Melani, and
L Cecchi, and
G Palazzino, and
G Filacchioni, and
C Martini, and
E Pennacchi, and
A Lucacchini
June 2006,
Bioorganic & medicinal chemistry,
F Melani, and
L Cecchi, and
G Palazzino, and
G Filacchioni, and
C Martini, and
E Pennacchi, and
A Lucacchini
January 2016,
Organic & biomolecular chemistry,
