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Synthesis and Pharmacological Studies for New Benzotriazole and Dibenzodiazepine Derivatives as Antipsychotic Agents
Faculty
Pharmacy
Year:
2009
Type of Publication:
Article
Pages:
1445-1451
Authors:
El-Sabbagh, Osama I, El-Nabtity, Sameh M
Journal:
BULLETIN OF THE KOREAN CHEMICAL SOCIETY KOREAN CHEMICAL SOC
Volume:
30
Research Area:
Chemistry
ISSN
ISI:000268554800006
Keywords :
Benzotriazole, Dibenzodiazepine, Antipsychotic activity
Abstract:
New benzotriazoles (5-8) or dibenzodiazepine derivatives (11-18) were synthesized starting from 3-{[}(2-amino-4,5-disubstitutedphenyl)amino]-5,5-disubstitutedcyclohex-2 -enones(1-4)through internal coupling of their diazonium salts or internal Mannich reaction in the presence of aromatic aldehydes. Pharmacological evaluation of benzotriazole and dibenzodiazepine derivatives for their clozapine-like properties revealed that dibenzodiazepine I I bearing 4-bromophenyl group exhibited the same antipsychotic activity as the reference drug clozapine while the activity of benzotriazole 7 was 25\% lesser than that of clozapine. Moreover, compounds 7 and I I did not show significant CNS depressant activity as well as no or slight neurotoxicity on contrast to clozapine when tested in mice using forced swim, rotarod and horizontal screen tests.
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