In the previous communication [I ] we have described an original method for the synthesis of tetraamines of type I, in which the methylene groups in radical B are partly replaced by aromatic fragments:RI_.CHzAr.
A series of N-(thieno[2,3-b]pyridin-3-yl)cyanoacetamides were prepared by reaction of 3aminothieno[2,3-b]pyridines with 1-cyanoacetyl-3,5-dimethytlpyrazole. Upon treatment with alkali, N-(2-alkoxycarbonylthieno[2,3-b]pyridin-3-yl)cyanoacetamides undergo Camps-type cyclization to give dipyridothiophenes. The relative stability of their tautomers was estimated by quantum chemical calculations. In contrast, cyclization of 3-(2-cyanoacetamido)thieno[2,3b]pyridine-2-carboxamides lead to the formation of pyrido[3',2':4,5]thieno[3,2-d]pyrimidines.
To simulate a convulsive syndrome, phenylcarbamate was administered intraperitoneally at a dose of 1 mg/kg. Valproic acid aminoester (43 mg/kg), caramiphene (50 mg/kg), and diferidine (2 mg/kg) were investigated as potential anticonvulsant drugs. Blood and brain tissue for the determination of acetylcholinesterase (AСhE) were taken at 10, 30, 60 minutes, 6 and 24 hours after administration of the xenobiotic. In case of poisoning with reversible inhibitors of AChE and accumulation of acetylcholine in the CNS synapses (due to inhibition of AChE activity), only the initial manifestations of convulsive activity are caused, and other mechanisms not associated with AChE inhibition are responsible for the processes of further maintenance and recurrence of seizures.
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