Potential metabolites of a condensed 2,3-benzodiazepine derivative.
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.
Csuzdi
Emese
E
IVAX Drug Research Institute Ltd., H-1045 Budapest, Berlini u. 47-49, Hungary.
Migléczi
Katalin
K
Hazai
István
I
Berzsenyi
Pál
P
Pallagi
István
I
Horváth
Gyula
G
Lengyel
György
G
Sólyom
Sándor
S
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
D000927:Anticonvulsants; D018696:Neuroprotective Agents; D001569:Benzodiazepines; D018350:alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid