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Summary
Novelty: Omega azole derivatives are disclosed. They are said to be more effective in treating cognitive disorders, senile dementia, Alzheimer's disease and related disorders that the anxiolytic benzodiazepines.
Biology: Cognition amelioration activity was shown by the preferred compound in a light/dark box test according to the method of Barnes et al. (Pharmacol. Biochem. Behav. (1990) 35:955-962). The reversal of the learning period produced by scopolamine was totally blocked. Antidepressive activity was demonstrated by immobility times in the test according to Porsolt et al. (Arch. Int. Pharmacodyn. (1977) 229:327-336). Results show the specified compound had activity from immobility times of 87, 58 and 32 seconds for control, compound and Imipramine, respectively. Doses were 1 and 30mg/kg, ip for the compound and Imipramine.
Chemistry: Five syntheses by standard techniques are described, together with three examples of preparation of the compounds. Characterization is by mp, IR and NMR. The specified compound is 1H-pyrazole-4-chloro-1-[4-[4-(2-pyrimidinyl)-1-piperazinyl]-butyl] dihydrochloride.
Structure: 