title: Synthesis and benzodiazepine receptor activity of some 4,5-dihydro-1H-pyrazolo[4,3-c][1,8]naphthyridine derivatives.
abstract: The preparation of 5-substituted 1-aryl-4,5-dihydro-1H-pyrazolo[4,3- c][1,8] naphthyridines by reaction of 5-substituted 3-hydroxymethylene-2,3-dihydro-1,8-naphthyridin-4(1H)-ones with various phenylhydrazines is described. The benzodiazepine binding activity of these compounds was evaluated in vitro. Only the 5-methyl substituted derivatives showed affinity for the benzodiazepine receptor, with K1 values ranging from 2.9 to 0.195 microM for the para-phenyl substituted compounds. A hypothesis of interaction of these ligands with the receptor site is reported.
authors.affiliation: Istituto Chimica Farmaceutica e Tossicologica, Università di Pisa, Italy.
authors.forename: A
authors.initials: A
authors.lastname: Da Settimo
authors.forename: G
authors.initials: G
authors.lastname: Primofiore
authors.forename: F
authors.initials: F
authors.lastname: Da Settimo
authors.forename: F
authors.initials: F
authors.lastname: Simorini
authors.forename: P L
authors.initials: PL
authors.lastname: Barili
authors.forename: G
authors.initials: G
authors.lastname: Senatore
authors.forename: C
authors.initials: C
authors.lastname: Martini
authors.forename: A
authors.initials: A
authors.lastname: Lucacchini
mesh_terms: D000818:Animals; D002417:Cattle; D008024:Ligands; D009287:Naphthyridines / Q000138:chemical synthesis* / Q000378:metabolism; D011963:Receptors, GABA-A / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D008024:Ligands; D009287:Naphthyridines; D011963:Receptors, GABA-A