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Design, Synthesis and Evaluation of Benzothiazole Urea Derivatives as an Anticonvulsant Agent | Abstract

Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry

ISSN: 0975-413X

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Abstract

Design, Synthesis and Evaluation of Benzothiazole Urea Derivatives as an Anticonvulsant Agent

Author(s): Snehal D. Kachare, Kamalkishor G. Baheti, Qazi Yasar and Sampada S. Jangam

A series of 1-((-6-substituted-2-yl)-3-(4H-1,2,4 triazole-3-yl)urea 7a-f and (1-((3-(6-substituted-2-yl)ureido)methyl)cyclohexyl)acetic acid 8a-fwere designed, synthesized using appropriate synthetic route and screened for CNS depressant and anticonvulsant activities. The synthesized compounds were also analyzed for ADME properties. The results of In-Silico ADME Screening showed that compounds could be exploited as an oral drug candidate. Molecular docking studies were performed for all the synthesized compounds against γ-amino butyric acid amino transferase enzyme (1OHV), All the compounds exhibited docking score in the range of -7.5 to -8.4, among which compound 8c had shown the highest docking scores as compared to the standard drug phenytoin. Animal study for anticonvulsant indicated that compounds 7b, 7e and 8c were exhibited significant activity at a dose 200 mg/kg. All these compounds were also evaluated for CNS depressant activity using actophotometer. The results of CNS depressant and anticonvulsant activities and docking study showed that synthesized compounds had potential CNS depressant and anticonvulsant activities and can be further optimized and developed as a lead compound.


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