title: Synthesis, benzodiazepine receptor affinity and anticonvulsant activity of 5-H-indeno[1,2-c]pyridazine derivatives.
abstract: Title compounds 1-36 were synthesized by reacting hydrazine with aldol adducts obtained from ninhydrin and methyl or alpha methylene ketones and aldehydes. Some of them showed a low, but significant benzodiazepine receptor affinity whose variation was interpreted through a structure-activity relationships study based on qualitative correlations and Comparative Molecular Field Analysis (CoMFA). Some indeno-pyridazine derivatives were found to possess an interesting anticonvulsant activity which however does not seem simply related to the benzodiazepine receptor modulation.
authors.affiliation: Dipartimento Farmacochimico, Università degli Studi di Bari.
authors.forename: C
authors.initials: C
authors.lastname: Altomare
authors.forename: F
authors.initials: F
authors.lastname: Campagna
authors.forename: V
authors.initials: V
authors.lastname: Carta
authors.forename: S
authors.initials: S
authors.lastname: Cellamare
authors.forename: A
authors.initials: A
authors.lastname: Carotti
authors.forename: G
authors.initials: G
authors.lastname: Genchi
authors.forename: G
authors.initials: G
authors.lastname: De Sarro
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D001921:Brain / Q000378:metabolism; D007192:Indenes / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D008297:Male; D051379:Mice; D008811:Mice, Inbred DBA; D008928:Mitochondria / Q000378:metabolism; D008958:Models, Molecular; D011724:Pyridazines / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D017207:Rats, Sprague-Dawley; D011963:Receptors, GABA-A / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D000927:Anticonvulsants; D007192:Indenes; D011724:Pyridazines; D011963:Receptors, GABA-A