Synthesis and BZR affinity of pyrazolo[1,5-a]pyrimidine derivatives. Part 1: study of the structural features for BZR recognition.
Examination of the pharmacophoric points of the pyrazolo[1,5-a]pyrimidine derivatives, ligands for BZR, previously published led us to the design of a novel class of 3,6-diaryl-4,7-dihydro-pyrazolo[1,5-a]pyrimidin-7-ones and to determine the groups involved in the BZR recognition.
Selleri
S
S
Department of Pharmaceutical Sciences, University of Firenze, Florence, Italy. sell@farmfi.scifarm.unifi.it
Bruni
F
F
Costagli
C
C
Costanzo
A
A
Guerrini
G
G
Ciciani
G
G
Costa
B
B
Martini
C
C
D000345:Affinity Labels / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism*; D000818:Animals; D001665:Binding Sites; D015195:Drug Design; D058787:GABA-A Receptor Antagonists; D066298:In Vitro Techniques; D007700:Kinetics; D008024:Ligands; D008958:Models, Molecular; D008968:Molecular Conformation; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism*; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism*; D011963:Receptors, GABA-A / Q000378:metabolism*; D013329:Structure-Activity Relationship
D000345:Affinity Labels; D058787:GABA-A Receptor Antagonists; D008024:Ligands; D011720:Pyrazoles; D011743:Pyrimidines; D011963:Receptors, GABA-A