Anticonvulsant activity and inhibition of cellular respiratory activity by substituted imidazolocarbamides.
Several 1-(1-aryl-2-mercaptoacetylimidazole)-3-alkylcarbamides were synthesized and characterized by their sharp melting points, elemental analyses, and IR spectra. These substituted imidazolocarbamides possessed anticonvulsant activity, which was reflected by the 20-80% protection observed with these compounds against pentylenetetrazol-induced convulsions in mice. These substituted imidazolocarbamides selectively inhibited the in vitro oxidation of nicotinamide adenine dinucleotide (NAD)-dependent oxidations of pyruvate, alpha-ketoglutarate, beta-hydroxybutyrate, and NADH by rat brain homogenates. However, NAD-independent oxidation of succinate was not affected. The anticonvulsant activity possessed by 1-(1-aryl-2-mercaptoacetylimidazole)-3-alkylcarbamides had no relationship to their ability to inhibit cellular respiratory activity.
D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology*; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D005260:Female; D007093:Imidazoles / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D010101:Oxygen Consumption / Q000187:drug effects*
D000927:Anticonvulsants; D007093:Imidazoles