title: Potential metabolites of a condensed 2,3-benzodiazepine derivative.
abstract: Putative metabolites of an AMPA antagonist imidazo-2,3-benzodiazepine (2) were synthesized and compared to constituents formed from the parent compound by a rat liver perfusion method. As metabolic transformations, hydroxylation of the 2-methyl group and N-acetylation of the amino functionality in parent compound (2) were registered. The hydroxylated analogue 12 of 2 exhibits a weak AMPA antagonist activity.
authors.affiliation: IVAX Drug Research Institute Ltd., H-1045 Budapest, Berlini u. 47-49, Hungary.
authors.forename: Emese
authors.initials: E
authors.lastname: Csuzdi
authors.forename: Katalin
authors.initials: K
authors.lastname: Migléczi
authors.forename: István
authors.initials: I
authors.lastname: Hazai
authors.forename: Pál
authors.initials: P
authors.lastname: Berzsenyi
authors.forename: István
authors.initials: I
authors.lastname: Pallagi
authors.forename: Gyula
authors.initials: G
authors.lastname: Horváth
authors.forename: György
authors.initials: G
authors.lastname: Lengyel
authors.forename: Sándor
authors.initials: S
authors.lastname: Sólyom
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000378:metabolism* / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D006900:Hydroxylation; D008099:Liver / Q000378:metabolism; D018696:Neuroprotective Agents / Q000138:chemical synthesis / Q000494:pharmacology; D010477:Perfusion; D051381:Rats; D013329:Structure-Activity Relationship; D018350:alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid / Q000037:antagonists & inhibitors
chemical_list: D000927:Anticonvulsants; D018696:Neuroprotective Agents; D001569:Benzodiazepines; D018350:alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid